Dosing & Uses
Dosage Forms & Strengths
tablet
- 1mg
- 5mg
Renal Cell Carcinoma
Monotherapy
- Indicated for advanced renal cell carcinoma (RCC) in patients who failed 1 prior systemic therapy
- 5 mg PO BID initially
Combination therapy with avelumab
- Indicated in combination with avelumab for first-line treatment of advanced RCC
- Axitinib 5 mg PO BID, plus
- Avelumab 800 mg IV q2Weeks
- Continue until disease progression or unacceptable toxicity
- During combination therapy with avelumab, consider escalating dose of axitinib above 5 mg/dose in 2-week intervals or longer
- Refer the prescribing information of avelumab for dosing information
Combination therapy with pembrolizumab
- Indicated in combination with pembrolizumab for first-line treatment of advanced RCC
- Axitinib 5 mg PO BID, plus
- Pembrolizumab 200 mg IV q3Weeks or 400 mg IV q6Weeks
- Continue until disease progression or unacceptable toxicity
- During combination therapy with pembrolizumab, consider escalating dose of axitinib above 5 mg/dose in 6-week intervals or longer
- Refer the prescribing information of pembrolizumab for dosing information
Dosage Modifications
Dose increase or reduction based on individual safety and tolerability
Dose escalation
- Criteria: Tolerated for at least 2 consecutive weeks with no Grade >2 adverse reactions and are normotensive and not receiving antihypertension medications
- First dose increase: 7 mg PO BID
- Second dose increase: Using the same criteria, may further increase to 10 mg PO BID
Dose reduction
- Management of some adverse drug reactions may require temporary interruption or permanent discontinuation and/or dose reduction of therapy
- Current dose is 5 mg PO BID: Reduce 3 mg PO BID
- If additional dose reduction is required, reduce to 2 mg PO BID
Strong CYP3A4/5 inhibitors
- Avoid coadministration
- Use an alternative with no CYP3A4/5 inhibition potential
- Although dose adjustment has not been studied, if a strong CYP3A4/5 inhibitor must be coadministered, decrease dose of axitinib by ~50%
- Subsequent doses can be increased or decreased based on individual safety and tolerability
- If strong inhibitor is discontinued, resume axitinib dose (after 3-5 half-lives of the inhibitor) to before initiating the strong CYP3A4/5 inhibitor
Hepatotoxicity (combination with avelumab)
- Refer prescribing information for avelumab for dosage modifications
-
ALT or AST ≥3x to <5x ULN or total bilirubin ≥1.5x ULN but <3x ULN
- Withhold both axitinib and avelumab until these adverse reactions recover to Grade ≤1
- If persistent (>5 days), consider corticosteroid therapy (initial dose of 0.5-1 mg/kg/day) prednisone or equivalent followed by a taper
- Consider rechallenge with a single drug or sequential rechallenge with both drugs after recovery
- If rechallenging axitinib, consider dose reduction as listed above
-
ALT or AST ≥5x ULN or >3x ULN with concurrent total bilirubin ≥2x ULN or total bilirubin ≥3x ULN
- Permanently discontinue both axitinib and avelumab
- Consider corticosteroid therapy (initial dose 1-2 mg/kg/day prednisone or equivalent followed by a taper)
-
Hepatotoxicity (combination with pembrolizumab)
- Refer prescribing information for pembrolizumab for dosage modifications
-
ALT or AST ≥3x to <10x ULN without concurrent total bilirubin ≥2x ULN
- Withhold both axitinib and pembrolizumab until these adverse reactions recover to Grade ≤1
- Consider rechallenge with a single drug or sequential rechallenge with both drugs after recovery
- If rechallenging axitinib, consider dose reduction as listed above
-
ALT or AST ≥10x ULN or >3x ULN with concurrent total bilirubin ≥2x ULN
- Permanently discontinue both axitinib and pembrolizumab
- Consider corticosteroid therapy
Renal & Hepatic Impairment
Renal impairment
- No dedicated renal impairment trial has been conducted
- Based on population pharmacokinetic analyses, no significant difference in clearance observed in patients with pre-existing mild-to-severe renal impairment
Hepatic impairment
- Mild (Child-Pugh A): No adjustment of initial dose is required
- Moderate (Child-Pugh B): Decrease initial dose by ~50%; subsequent doses can be increased or decreased based on individual safety and tolerability
- Severe (Child-Pugh C): Has not been studied
<18 years: Safety and efficacy not established
In clinical trials, 34% of participants 65 years or older
No overall differences were observed in the safety or efficacy between elderly and younger patients
No dosage adjustment required in elderly patients
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (77)
- abametapir
abametapir increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.
- amiodarone
amiodarone increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- amobarbital
amobarbital will decrease the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- apalutamide
apalutamide will decrease the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.
- aprepitant
aprepitant increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- armodafinil
armodafinil decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.
- atazanavir
atazanavir increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%.
- bicalutamide
bicalutamide increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- bosentan
bosentan decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.
- carbamazepine
carbamazepine decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.
- cimetidine
cimetidine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- clarithromycin
clarithromycin increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%.
- clobazam
clobazam decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.
- clotrimazole
clotrimazole increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- clozapine
clozapine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- cobicistat
cobicistat will increase the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- conivaptan
conivaptan increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%.
- cyclosporine
cyclosporine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- darunavir
darunavir increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%.
- desipramine
desipramine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- dexamethasone
dexamethasone decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.
- doxycycline
doxycycline increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- dronedarone
dronedarone increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- efavirenz
efavirenz decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.
- enzalutamide
enzalutamide will decrease the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- erythromycin base
erythromycin base increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- erythromycin ethylsuccinate
erythromycin ethylsuccinate increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- erythromycin lactobionate
erythromycin lactobionate increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- erythromycin stearate
erythromycin stearate increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended
- etravirine
etravirine decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.
- fexinidazole
fexinidazole will increase the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.
- fluconazole
fluconazole increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- fosamprenavir
fosamprenavir increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%.
- fosphenytoin
fosphenytoin decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.
- grapefruit
grapefruit increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- haloperidol
haloperidol increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- idelalisib
idelalisib will increase the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Idelalisib is a strong CYP3A inhibitor; avoid coadministration with sensitive CYP3A substrates
- imatinib
imatinib increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%.
- indinavir
indinavir increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%.
- isoniazid
isoniazid increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%.
- itraconazole
itraconazole increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%.
- ivosidenib
ivosidenib will decrease the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternate therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.
- ketoconazole
ketoconazole increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%. If strong CYP3A4 inhibitor is discontinued, axitinib dose should changed (after 3-5 half lives of the inhibitor) to that used before initiating the inhibitor.
- lapatinib
lapatinib increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- lidocaine
lidocaine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- lonafarnib
lonafarnib will increase the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration with sensitive CYP3A substrates. If coadministration unavoidable, monitor for adverse reactions and reduce CYP3A substrate dose in accordance with product labeling.
- lopinavir
lopinavir increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%.
- lorlatinib
lorlatinib will decrease the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- metronidazole
metronidazole increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- nafcillin
nafcillin decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.
- nefazodone
nefazodone increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%.
- nelfinavir
nelfinavir increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%.
- nevirapine
nevirapine decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.
- nicardipine
nicardipine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%.
- oxcarbazepine
oxcarbazepine decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.
- palifermin
palifermin increases toxicity of axitinib by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hr before, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.
- pentobarbital
pentobarbital decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.
- phenobarbital
phenobarbital decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.
- phenytoin
phenytoin decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.
- posaconazole
posaconazole increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%.
- primidone
primidone decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.
- quinidine
quinidine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%.
- rifabutin
rifabutin decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.
- rifampin
rifampin decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.
- rifapentine
rifapentine decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.
- ritonavir
ritonavir increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%.
- saquinavir
saquinavir increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%.
- secobarbital
secobarbital will decrease the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- sertraline
sertraline increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- St John's Wort
St John's Wort decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Selection of concomitant medication with no or minimal CYP3A4 induction potential is recommended.
- tetracycline
tetracycline increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- tipranavir
tipranavir increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%.
- tucatinib
tucatinib will increase the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.
- verapamil
verapamil increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- voriconazole
voriconazole increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with strong CYP3A4 inhibitors, reduce axitinib dose by 50%.
- voxelotor
voxelotor will increase the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.
Monitor Closely (148)
- acetaminophen
acetaminophen increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- acetaminophen IV
acetaminophen IV increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- acetaminophen rectal
acetaminophen rectal increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- acetazolamide
acetazolamide increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- amlodipine
amlodipine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- anastrozole
anastrozole increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- artesunate
axitinib will increase the level or effect of artesunate by decreasing metabolism. Use Caution/Monitor. Coadministration may increase active artesunate metabolite (DHA) by inhibiting UGT. Monitor for increased adverse effects.
- atorvastatin
atorvastatin increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- azelastine
azelastine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- bazedoxifene/conjugated estrogens
bazedoxifene/conjugated estrogens decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- belzutifan
belzutifan will decrease the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If unable to avoid coadministration of belzutifan with sensitive CYP3A4 substrates, consider increasing the sensitive CYP3A4 substrate dose in accordance with its prescribing information.
- betamethasone
betamethasone increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- betamethasone topical
betamethasone topical increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- bexarotene
bexarotene decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- bortezomib
bortezomib increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- bromocriptine
bromocriptine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- calcitriol
calcitriol decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- cenobamate
cenobamate will decrease the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.
- chloramphenicol
chloramphenicol increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- chlorzoxazone
chlorzoxazone increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ciprofloxacin
ciprofloxacin increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- clemastine
clemastine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- cocaine
cocaine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- colchicine
colchicine decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- conjugated estrogens
conjugated estrogens decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- conjugated estrogens, vaginal
conjugated estrogens, vaginal decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- crofelemer
crofelemer increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Crofelemer has the potential to inhibit CYP3A4 at concentrations expected in the gut; unlikely to inhibit systemically because minimally absorbed.
- cyclophosphamide
cyclophosphamide increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- dabrafenib
dabrafenib will decrease the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- danazol
danazol increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- darifenacin
darifenacin increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- dasatinib
dasatinib increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- deferasirox
deferasirox decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- desvenlafaxine
desvenlafaxine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- dexmedetomidine
dexmedetomidine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- diazepam
diazepam increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- diclofenac
diclofenac increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- diclofenac topical
diclofenac topical increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- dicloxacillin
dicloxacillin decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- dihydroergotamine
dihydroergotamine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- dihydroergotamine intranasal
dihydroergotamine intranasal increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- diltiazem
diltiazem increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- disulfiram
disulfiram increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- docetaxel
docetaxel increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- doxorubicin
doxorubicin increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- doxorubicin liposomal
doxorubicin liposomal increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- drospirenone
drospirenone increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- duvelisib
duvelisib will increase the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. will increase the level or effect of
- elagolix
elagolix will decrease the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Cobicistat is a CYP3A4 inhibitor; contraindicated with CYP3A4 substrates for which elevated plasma concentrations are associated with serious and/or life-threatening events.
- encorafenib
encorafenib, axitinib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.
- ergotamine
ergotamine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- esomeprazole
esomeprazole will increase the level or effect of axitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.
- estradiol
estradiol decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- estrogens conjugated synthetic
estrogens conjugated synthetic decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ethinylestradiol
ethinylestradiol increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- etoposide
etoposide increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- fedratinib
fedratinib will increase the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.
- felbamate
felbamate decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- felodipine
felodipine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- fluoxetine
fluoxetine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- fluvastatin
fluvastatin increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- fluvoxamine
fluvoxamine will increase the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- glyburide
glyburide increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- griseofulvin
griseofulvin decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- hydralazine
hydralazine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- hydrocortisone
hydrocortisone decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- hydrocortisone topical
hydrocortisone topical decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ifosfamide
ifosfamide increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- iloperidone
iloperidone increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Iloperidone is a time-dependent CYP3A inhibitor and may lead to increased plasma levels of drugs predominantly eliminated by CYP3A4.
- irbesartan
irbesartan increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- isradipine
isradipine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- istradefylline
istradefylline will increase the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.
- lansoprazole
lansoprazole increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- losartan
losartan increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lovastatin
lovastatin increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lurasidone
lurasidone increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- medroxyprogesterone
medroxyprogesterone decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- mefloquine
mefloquine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- mestranol
mestranol increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- methadone
methadone increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- methimazole
methimazole increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- methoxsalen
methoxsalen increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- methylprednisolone
methylprednisolone increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- metyrapone
metyrapone decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- micafungin
micafungin increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- midazolam
midazolam increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- mifepristone
mifepristone increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- mirtazapine
mirtazapine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- mitotane
mitotane decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Mitotane is a strong inducer of cytochrome P-4503A4; monitor when coadministered with CYP3A4 substrates for possible dosage adjustments.
- mitoxantrone
mitoxantrone increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- modafinil
modafinil decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nifedipine
nifedipine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nisoldipine
nisoldipine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nizatidine
nizatidine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- olanzapine
olanzapine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- omeprazole
omeprazole increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- orphenadrine
orphenadrine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- oxybutynin
oxybutynin increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- oxybutynin topical
oxybutynin topical increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- oxybutynin transdermal
oxybutynin transdermal increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- paclitaxel
paclitaxel decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- paclitaxel protein bound
paclitaxel protein bound decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- paroxetine
paroxetine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- pazopanib
pazopanib increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- pentamidine
pentamidine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- pilocarpine
pilocarpine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- pimozide
pimozide increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- pioglitazone
pioglitazone decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- pravastatin
pravastatin increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- prednisone
prednisone decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- primaquine
primaquine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- progesterone intravaginal gel
progesterone intravaginal gel increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- progesterone micronized
progesterone micronized increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- progesterone, natural
progesterone, natural increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- propofol
propofol increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- quinine
quinine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- rabeprazole
rabeprazole increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ranolazine
ranolazine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ribociclib
ribociclib will increase the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- risperidone
risperidone increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- rucaparib
rucaparib will increase the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.
- selegiline
selegiline increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- siponimod
siponimod and axitinib both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.
- sirolimus
sirolimus increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- sodium zirconium cyclosilicate
sodium zirconium cyclosilicate will decrease the level or effect of axitinib by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Check specific recommendations for drugs that exhibit pH-dependent solubility that may affect their systemic exposure and efficacy. In general, administer drugs at least 2 hr before or after sodium zirconium cyclosilicate.
- stiripentol
stiripentol, axitinib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.
- sulconazole
sulconazole increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tacrolimus ointment
tacrolimus ointment increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tamoxifen
tamoxifen increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tazemetostat
tazemetostat will decrease the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tecovirimat
tecovirimat will decrease the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.
- temsirolimus
temsirolimus increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- teniposide
teniposide increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- testosterone
testosterone increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- testosterone buccal system
testosterone buccal system increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- testosterone topical
testosterone topical increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ticlopidine
ticlopidine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- topiramate
topiramate decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tranylcypromine
tranylcypromine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- trazodone
trazodone increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- valproic acid
valproic acid increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- vinblastine
vinblastine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- vincristine
vincristine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- vincristine liposomal
vincristine liposomal increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- vinorelbine
vinorelbine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- zafirlukast
zafirlukast increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ziprasidone
ziprasidone increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
Minor (3)
- dexlansoprazole
dexlansoprazole will decrease the level or effect of axitinib by increasing gastric pH. Applies only to oral form of both agents. Minor/Significance Unknown.
- famotidine
famotidine will decrease the level or effect of axitinib by increasing gastric pH. Applies only to oral form of both agents. Minor/Significance Unknown.
- ibuprofen/famotidine
ibuprofen/famotidine will decrease the level or effect of axitinib by increasing gastric pH. Applies only to oral form of both agents. Minor/Significance Unknown.
Adverse Effects
>10%
Diarrhea (55%)
Hypertension (40%)
Fatigue (39%)
Decreased appetite (34%)
Nausea (32%)
Dysphonia (31%)
Palmar-plantar erythrodysesthesia syndrome (27%)
Weight decreased (25%)
Vomiting (24%)
Asthenia (21%)
Constipation (20%)
Hypothyroidism (19%)
Cough (15%)
Mucosal inflammation (15%)
Arthralgia (15%)
Stomatitis (15%)
Dyspnea (15%)
Abdominal pain (14%)
Headache (14%)
Extremity pain (13%)
Rash (13%)
Proteinuria (11%)
Dysgeusia (11%)
1-10%
Dry skin (10%)
Dyspepsia (10%)
Dizziness (9%)
Upper abdominal pain (8%)
Myalgia (7%)
Pruritus (7%)
Dehydration (6%)
Epistaxis (6%)
Hypercalcemia (6%)
Anemia (4%)
Alopecia (4%)
Hemorrhoids (4%)
Hematuria (3%)
Tinnitus (3%)
Increased lipase (3%)
Glossodynia (3%)
Pulmonary embolism (2%)
Rectal hemorrhage (2%)
Hemoptysis (2%)
Erythema (2%)
DVT (1%)
Retinal vein occlusion/thrombosis (1%)
Polycythemia (1%)
TIA (1%)
<1%
Reversible posterior leukoencephalopathy syndrome
Postmarketing Reports
Vascular disorders: Arterial (including aortic) aneurysms, dissections, and rupture
Warnings
Contraindications
None
Cautions
Hypertension and hypertensive crisis reported in clinical trials, typically within the first month of treatment; blood pressure increases may appear as early as 4 days after initiating; blood pressure should be well controlled before starting therapy; dosage modification or discontinuation of treatment may be required (see Dosage Modification)
Although rare, arterial thromboembolic events (including deaths) reported during clinical trials
Venous thromboembolic events (eg, DVT, PE, retinal vein occlusion, retinal vein thrombosis) reported, including deaths
Hemorrhagic events (eg, cerebral hemorrhage, hematuria, hemoptysis, GI bleeding, melena) may occur
Rare occurrences of GI perforation and fistula formation reported
May cause thyroid dysfunction; monitor thyroid function before initiating and periodically throughout therapy
Stop treatment 24 hr before scheduled surgery
May cause proteinuria; monitor proteinuria before initiating and periodically throughout therapy
Elevated liver enzymes reported; monitor ALT, AST, and bilirubin
Moderate hepatic impairment requires dose reduction (see Dosage modification)
Coadministration with strong CYP3A4/5 inhibitors or inducers should be avoided if possible (see Dosage modifications)
Cardiac failure reported with axitinib use; monitor for signs or symptoms of cardiac failure throughout treatment; may require permanent discontinuation of axitinib
Impaired wound healing
- Impaired wound healing can occur in patients who receive drugs that inhibit the vascular endothelial growth factor (VEGF) signaling pathway
- Therefore axitinib has the potential to adversely affect wound healing
- Withhold for at least 2 days prior to elective surgery; do not administer for at least 2 weeks following major surgery and until adequate wound healing
- Safety of resumption after resolution of wound healing complications has not been established
Major adverse cardiovascular events (MACE)
- Combination therapy with avelumab may cause severe and fatal cardiovascular events
- Consider baseline and periodic evaluations of left ejection fraction; monitor signs and symptoms of cardiovascular events
- Optimize management of cardiovascular risk factors, such as hypertension, diabetes, or dyslipidemia
- Discontinue axitinib and avelumab for Grade 3-4 cardiovascular events
In combination with avelumab or with pembrolizumab
- Combination with avelumab or with pembrolizumab can cause hepatotoxicity with higher than expected frequencies of Grade 3 and 4 ALT and AST elevation; consider more frequent monitoring of liver enzymes as compared to when drugs are used as monotherapy
- Withhold axitinib and avelumab for moderate (Grade 2) hepatotoxicity and permanently discontinue the combination for severe or life-threatening (Grade 3 or 4) hepatotoxicity; administer corticosteroids as needed
- For elevated liver enzymes, interrupt axitinib and pembrolizumab and consider administering corticosteroids as needed
Pregnancy & Lactation
Pregnancy
Based on mechanism of action and findings from animal studies, drug can cause fetal harm when administered to a pregnant woman; there are no available human data to inform drug-associated risk; in developmental toxicity studies in mice, axitinib was teratogenic, embryotoxic and fetotoxic at maternal exposures that were lower than human exposures at recommended clinical dose
When used in combination with avelumab or pembrolizumab, refer to full prescribing information of avelumab or pembrolizumab for pregnancy information
Animal data
- Therapy administered twice daily to female mice prior to mating and through first week of pregnancy caused increase in post-implantation loss at all doses tested (greater than or equal 15 mg/kg/dose, approximately 10 times the systemic exposure (AUC) in patients at recommended starting dose)
- Based on findings in animal studies, drug can cause fetal harm when administered to a pregnant woman; females of reproductive potential should have a pregnancy test prior to starting treatment
Contraception
- Females: Therapy can cause fetal harm when administered to a pregnant woman; advise females of reproductive potential to use effective contraception during treatment and for 1 week after last dose
- Males: Based on findings in animal studies, advise males with female partners of reproductive potential to use effective contraception during treatment and for 1 week after last dose
- When is used in combination with avelumab or pembrolizumab, refer to the full prescribing information of avelumab or pembrolizumab for contraception information
Infertility
- Based on findings in animals, therapy may impair fertility in females and males of reproductive potential
Lactation
There are no data on presence of drug in human milk, or effects on breastfed child or on milk production; because of potential for serious adverse reactions in a breastfed child, advise lactating women not to breastfeed during treatment and for 2 weeks after final dose
When used in combination with avelumab or pembrolizumab, refer to full prescribing information of avelumab or pembrolizumab for lactation information
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Multi-targeted tyrosine kinase inhibitor
Inhibits receptor tyrosine kinases including vascular endothelial growth factor receptors (VEGFR)-1, VEGFR-2, and VEGFR-3
Absorption
Bioavailability: 58%
Peak Plasma Time: 2.5-4.1 hr
Peak Plasma Concentration: 27.8 ng/mL
AUC: 265 ng•h/mL
Distribution
Protein Bound: >99% (mostly to albumin, moderately to alpha1-acid glycoprotein)
Vd: 160 L
Metabolism
Metabolized primarily by CYP3A4/5 and to a lesser degree by CYP1A2, CYP2C19, and UGT1A1
Metabolites: Plasma levels detected the N-glucuronide metabolite (50%), sulfoxide metabolite (20%), and 20% unchanged drug
Elimination
Half-life: 2.5-6.1
Total body clearance: 38 L/h
Excretion: feces 41% (12% unchanged), urine 23% (as carboxylic acid and sulfoxide metabolites)
Administration
Oral Administration
Administer twice daily ~12 hr apart
May be taken with or without food
Swallow tablet whole with a glass of water; do not split, crush, or chew
If patient vomits or misses a dose, an additional dose should not be taken; the next prescribed dose should be taken at the usual time
Storage
Store at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86°F)
Images
Patient Handout
axitinib oral
AXITINIB - ORAL
(ax-I-ti-nib)
COMMON BRAND NAME(S): Inlyta
USES: This medication is used to treat kidney cancer. Axitinib works by slowing or stopping the growth of cancer cells. It belongs to a class of drugs known as tyrosine kinase inhibitors.
HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start using axitinib and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with or without food as directed by your doctor, usually two times daily, about 12 hours apart. Swallow the tablet whole with a glass of water. Do not split or crush this medication.Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor or pharmacist says you may do so safely. Grapefruit can increase the chance of side effects with this medicine. Ask your doctor or pharmacist for more details.The dosage is based on your medical condition, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products). If you have certain side effects, your doctor may adjust your dose or stop treatment for some time.Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of serious side effects will increase.If you vomit your dose of axitinib, do not take an additional dose. Take your next dose at your regular scheduled time. Do not take two doses at the same time.Take this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.
SIDE EFFECTS: Nausea, vomiting, loss of appetite, dizziness, tiredness/weakness, weight loss, temporary hair loss, cough, headache, altered sense of taste, hoarseness, constipation, or upset stomach may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.Diarrhea is a common side effect that can cause dehydration. Drink plenty of fluids to reduce the risk of dehydration. Tell your doctor right away if you develop signs of dehydration (such as dizziness/lightheadedness, unusual dry mouth/thirst).Axitinib may cause a rash that is usually not serious. Mild to moderate skin reactions include dry skin or a mildly red/itchy rash. However, you may not be able to tell it apart from a rash that could be a sign of a severe reaction. Tell your doctor right away if you develop any rash.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: signs of kidney problems (such as change in the amount of urine, foamy urine), muscle/joint pain, swelling of ankles/feet/hands, unusual tiredness, shortness of breath, easy bruising or bleeding (such as nose/gum bleeds, pink/dark urine), burning/sores/pain in the mouth or throat, redness/blisters/swelling/pain on the palms of your hands or soles of your feet, slow wound healing, signs of an abnormal thyroid (such as unusual weight gain/loss, cold/heat intolerance, slow/fast/irregular heartbeat, unusual tiredness), signs of liver problems (such as nausea/vomiting that doesn't stop, loss of appetite, stomach/abdominal pain, yellowing eyes/skin, dark urine).This medication may lower your ability to fight infections. This may make you more likely to get a serious infection or make any infection you have worse. Tell your doctor right away if have any signs of infection (such as fever, chills, persistent sore throat).This medication may raise your blood pressure. Check your blood pressure regularly and tell your doctor if the results are high. Your doctor may control your blood pressure with medication.Rarely, axitinib may cause a condition known as RPLS (reversible posterior leukoencephalopathy syndrome). Get medical help right away if you develop persistent headache, seizures, sudden vision changes, mental/mood changes (such as confusion).This medication may rarely cause serious (possibly fatal) blood clots (such as stroke/TIA, heart attack, pulmonary embolism, deep vein thrombosis, retinal vein/artery occlusion). You may be at increased risk for blood clots if you are severely dehydrated, or have a history of blood clots, heart/blood vessel disease, heart failure, stroke, or if you are immobile (such as on very long plane flights or being bedridden). If you use estrogen-containing products, these may also increase your risk. Before using this medication, if you have any of these conditions report them to your doctor or pharmacist. Get medical help right away if any of these side effects occur: shortness of breath/rapid breathing, chest/jaw/left arm pain, unusual sweating, confusion, sudden dizziness/fainting, pain/swelling/warmth in the groin/calf, sudden severe headaches, trouble speaking, weakness on one side of the body, sudden vision changes.Get medical help right away if you have any very serious side effects, including: severe persistent stomach/abdominal pain, signs of bleeding (such as bloody/black stools, vomit that looks like coffee grounds, coughing/vomiting up blood), sudden/severe back pain.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: See also Side Effects section.Before taking axitinib, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, kidney disease, high blood pressure, bleeding/clotting problems (such as bleeding from intestinal/stomach ulcers), blood vessel problems (such as an aneurysm or a tear/break in the aorta or other blood vessels), heart problems (such as heart failure, previous heart attack), thyroid problems.Axitinib can make you more likely to get infections or may worsen any current infections. Avoid contact with people who have infections that may spread to others (such as chickenpox, measles, flu). Consult your doctor if you have been exposed to an infection or for more details.Tell your health care professional that you are using axitinib before having any immunizations/vaccinations. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).This drug may make you dizzy. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products). Axitinib should be stopped at least 2 days before planned surgery.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.Tell your doctor if you are pregnant or plan to become pregnant. You should not become pregnant while using axitinib. Axitinib may harm an unborn baby. Women of childbearing age and men should ask about reliable forms of birth control while using this medication and for at least 1 week after stopping treatment. If you or your partner becomes pregnant, talk to the doctor right away about the risks and benefits of this medication.It is unknown if this drug passes into breast milk. Because of the possible risk to the infant, breast-feeding is not recommended while using this medication and for at least 2 weeks after stopping treatment. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Other medications can affect the removal of axitinib from your body, which may affect how axitinib works. Examples include rifamycins (such as rifampin, rifabutin, rifapentine), drugs to treat seizures (such as phenytoin, carbamazepine, phenobarbital), St. John's wort, bosentan, efavirenz, modafinil, nafcillin, etravirine, dexamethasone, among others.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: seizures, extreme dizziness, extreme/persistent headache, vomiting blood.
NOTES: Do not share this medication with others.Lab and/or medical tests (such as blood pressure, thyroid/kidney/liver/pancreatic function tests, complete blood counts, urine tests, blood mineral levels including sodium/potassium) should be done while you are taking this medication. Women of childbearing age should have a pregnancy test before starting axitinib. Keep all medical and lab appointments.
MISSED DOSE: It is important to get each dose of this medication as scheduled. If you miss a dose, ask your doctor or pharmacist right away for a new dosing schedule. Do not double the dose to catch up.
STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).
Information last revised November 2021. Copyright(c) 2021 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
