Dosing & Uses
Dosage Forms & Strengths
tablet
- 25mg
- 100mg
Acute Myeloid Leukemia
Indicated, in combination with low-dose cytarabine, for newly diagnosed acute myeloid leukemia (AML) in adults aged ≥75 years or who have comorbidities that preclude use of intensive induction chemotherapy
100 mg PO qDay on days 1-28 of each 28-day cycle; administer in combination with cytarabine 20 mg SC BID on days 1-10
For patients without unacceptable toxicity, treat for a minimum of 6 cycles to allow time for clinical response
Dosage Modifications
QT prolongation (≥2 separate ECGs)
-
QTc >480 to 500 ms
- Assess electrolyte levels and supplement as clinically indicated
- Review and adjust concomitant medications with known QTc interval-prolonging effects
- Monitor ECGs at least weekly for 2 weeks following QTc prolongation resolution to ≤480 ms
-
QT >500 ms
- Assess electrolyte levels and supplement as clinically indicated
- Review and adjust concomitant medications with known QTc interval-prolonging effects
- Interrupt glasdegib dosing; resume at reduced dose of 50 mg qDay when QTc interval returns to within 30 ms of baseline or ≤480 ms
- Monitor ECGs at least weekly for 2 weeks following QTc prolongation resolution
- Consider re-escalating glasdegib dose to 100 mg qDay if other etiology identified for QTc prolongation
-
QTc prolongation with life-threatening arrhythmia
- Discontinue permanently
Hematologic toxicity
- Platelets <10 Gi/L or neutrophil count <0.5 Gi/L for >42 days in absence of disease: Discontinue glasdegib and cytarabine permanently
Nonhematologic toxicity
-
Grade 3
- Interrupt glasdegib and/or cytarabine until symptoms reduce to mild or return to baseline
- Resume glasdegib at the same dose level, or reduce dose to 50 mg
- Resume cytarabine at the same dose level, or reduce dose to 15 mg or 10 mg
- If toxicity recurs, discontinue glasdegib and cytarabine
- If toxicity attributed only to glasdegib, cytarabine may be continued
-
Grade 4
- Discontinue glasdegib and cytarabine permanently
Strong or moderate CYP3A4 inducers
- Avoid; coadministration may decrease glasdegib plasma concentrations, thereby reducing efficacy
- May increase glasdegib dose if coadministration with moderate CYP3A4 inducers cannot be avoided
-
Glasdegib dose adjustment if coadministration with moderate CYP3A4 inducer
- If taking 100 mg/day: Increase to 200 mg PO qDay
- If taking 50 mg/day: Increase to 100 mg PO qDay
- After moderate CYP3A4 inducer discontinued for 7 days, resume previous glasdegib dose
Renal impairment
- Mild-to-severe (eGFR 15-89 mL/min): No dosage modifications recommended
- Monitor patients with severe renal impairment (eGFR 15-29 mL/min) for increased risk of adverse effects including QTc prolongation owing to increased serum levels
Hepatic impairment
- Not studied
Dosing Considerations
Limitations of use: Not studied in patients with severe renal impairment or moderate-to-severe hepatic impairment
Conduct pregnancy testing in females of reproductive potential before initiating
Monitoring
- Assess complete blood cell counts, electrolytes, renal function, and hepatic function before initiating and at least once weekly for the first month
- Monitor electrolytes and renal function once monthly for the duration of therapy
- Obtain serum creatine kinase levels before initiating and as indicated clinically thereafter (eg, if muscle symptoms are reported)
- Monitor ECG) before initiating, ~1 week after initiation, and then once monthly for the next 2 months to assess for QTc prolongation; repeat ECG if abnormal; certain patients may require more frequent and ongoing ECG monitoring
Safety and efficacy not established
See adult dosing
Of the total number of patients in clinical trials, 98% were aged ≥65 years and 60% were aged ≥75 years
There were insufficient patients younger than age 65 years to determine differences in adverse reactions reported from patients older than 65 years
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (1)
- lefamulin
lefamulin will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Lefamulin is contraindicated with CYP3A substrates know to prolong the QT interval.
Serious - Use Alternative (174)
- abametapir
abametapir will increase the level or effect of glasdegib 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.
- adagrasib
adagrasib, glasdegib. Either increases effects of the other by QTc interval. Avoid or Use Alternate Drug. Each drug prolongs the QTc interval, which may increased the risk of Torsade de pointes, other serious arryhthmias, and sudden death. If coadministration unavoidable, more frequent monitoring is recommended for such patients.
- alfuzosin
alfuzosin and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- amiodarone
amiodarone and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- amisulpride
amisulpride and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. ECG monitoring is recommended if coadministered.
- amobarbital
amobarbital will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- anagrelide
anagrelide and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- apalutamide
apalutamide will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- apomorphine
apomorphine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- arformoterol
arformoterol and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- aripiprazole
aripiprazole and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- arsenic trioxide
arsenic trioxide and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- artemether
artemether and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- artemether/lumefantrine
artemether/lumefantrine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- asenapine
asenapine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- asenapine transdermal
asenapine transdermal and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- atazanavir
atazanavir will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
- atomoxetine
atomoxetine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- azithromycin
azithromycin and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- bedaquiline
bedaquiline and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- belzutifan
belzutifan will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration of belzutifan with sensitive CYP3A4 substrates, consider increasing the sensitive CYP3A4 substrate dose in accordance with its prescribing information.
- bosentan
bosentan will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- buprenorphine
buprenorphine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine buccal
buprenorphine buccal and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine subdermal implant
buprenorphine subdermal implant and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine transdermal
buprenorphine transdermal and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine, long-acting injection
buprenorphine, long-acting injection and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- butabarbital
butabarbital will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- butalbital
butalbital will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- carbamazepine
carbamazepine will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- ceritinib
ceritinib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
ceritinib will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - chloramphenicol
chloramphenicol will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
- chloroquine
chloroquine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- chlorpromazine
chlorpromazine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- ciprofloxacin
ciprofloxacin and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- citalopram
citalopram and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- clarithromycin
clarithromycin will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
clarithromycin and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation. - clofazimine
clofazimine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- clozapine
clozapine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- cobicistat
cobicistat will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
- conivaptan
conivaptan will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
- crizotinib
crizotinib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- dabrafenib
dabrafenib will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- darunavir
darunavir will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
- dasatinib
dasatinib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- degarelix
degarelix and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- desflurane
desflurane and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- disopyramide
disopyramide and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- dofetilide
dofetilide and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- dolasetron
dolasetron and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- donepezil
donepezil and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- doxepin
doxepin and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- dronedarone
dronedarone and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- droperidol
droperidol and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- efavirenz
efavirenz will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
efavirenz and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation. - eliglustat
eliglustat and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
- encorafenib
encorafenib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- entrectinib
glasdegib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
- enzalutamide
enzalutamide will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- eribulin
eribulin and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- erythromycin base
erythromycin base and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- erythromycin ethylsuccinate
erythromycin ethylsuccinate and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- erythromycin lactobionate
erythromycin lactobionate and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- erythromycin stearate
erythromycin stearate and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- escitalopram
escitalopram and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- etravirine
etravirine will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- ezogabine
ezogabine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- fexinidazole
fexinidazole and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of fexinidazole with drugs known to block potassium channels and/or prolong QT interval.
- fingolimod
fingolimod and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- flecainide
flecainide and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- fluconazole
fluconazole and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- fluoxetine
fluoxetine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- formoterol
formoterol and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- fosphenytoin
fosphenytoin will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- gemifloxacin
gemifloxacin and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- gemtuzumab
gemtuzumab and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- gilteritinib
gilteritinib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- goserelin
goserelin and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- granisetron
granisetron and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- grapefruit
grapefruit will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
- haloperidol
haloperidol and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- histrelin
histrelin and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- hydroxychloroquine sulfate
hydroxychloroquine sulfate and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- hydroxyzine
hydroxyzine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- ibutilide
ibutilide and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- idelalisib
idelalisib will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
- iloperidone
iloperidone and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- imatinib
imatinib will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
- indacaterol, inhaled
indacaterol, inhaled and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- indinavir
indinavir will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
- inotuzumab
inotuzumab and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- isoflurane
isoflurane and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- isoniazid
isoniazid will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
- itraconazole
itraconazole and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- ivosidenib
ivosidenib will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- ketoconazole
ketoconazole will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
- lapatinib
lapatinib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- lenvatinib
lenvatinib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- leuprolide
leuprolide and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- levofloxacin
levofloxacin and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- levoketoconazole
levoketoconazole will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
- lithium
lithium and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- lofexidine
lofexidine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- lopinavir
lopinavir will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
lopinavir and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation. - lorlatinib
lorlatinib will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- lumacaftor/ivacaftor
lumacaftor/ivacaftor will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- methadone
methadone and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- mifepristone
mifepristone will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
mifepristone and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation. - mirtazapine
mirtazapine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- mitotane
mitotane will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- moxifloxacin
moxifloxacin and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- nafcillin
nafcillin will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- nefazodone
nefazodone will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
- nelfinavir
nelfinavir will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
- nilotinib
nilotinib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- ofloxacin
ofloxacin and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- olanzapine
olanzapine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- ondansetron
ondansetron and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- osimertinib
osimertinib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- oxaliplatin
oxaliplatin and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- paliperidone
paliperidone and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- panobinostat
panobinostat and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- pasireotide
pasireotide and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- pazopanib
pazopanib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- pentamidine
pentamidine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- pentobarbital
pentobarbital will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- phenobarbital
phenobarbital will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- phenytoin
phenytoin will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- pimavanserin
pimavanserin and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- pimozide
pimozide and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- pitolisant
glasdegib and pitolisant both increase QTc interval. Avoid or Use Alternate Drug.
- posaconazole
posaconazole will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
- primaquine
primaquine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- primidone
primidone will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- procainamide
procainamide and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- propafenone
propafenone and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- quetiapine
quetiapine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- quinidine
quinidine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- quinine
quinine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- ranolazine
ranolazine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- ribociclib
ribociclib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- rifabutin
rifabutin will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- rifampin
rifampin will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- rifapentine
rifapentine will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- risperidone
risperidone and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- ritonavir
ritonavir will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
- romidepsin
romidepsin and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- saquinavir
saquinavir will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
saquinavir and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation. - secobarbital
secobarbital will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- sertraline
sertraline and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- sevoflurane
sevoflurane and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- siponimod
siponimod and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- solifenacin
solifenacin and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- sorafenib
sorafenib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- sotalol
sotalol and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- St John's Wort
St John's Wort will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glasdegib with strong CYP3A inducers.
- stiripentol
stiripentol, glasdegib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Stiripentol may either inhibit or induce CYP3A4. Monitor glasdegib for decreased efficacy or increased risk of adverse effects, including QTc interval prolongation. Dosage adjustment may be needed.
- sunitinib
sunitinib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- tacrolimus
tacrolimus and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- telavancin
telavancin and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- tetrabenazine
tetrabenazine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- thioridazine
thioridazine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- tipranavir
tipranavir will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
- toremifene
toremifene and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- trazodone
trazodone and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- triptorelin
triptorelin and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- tucatinib
tucatinib will increase the level or effect of glasdegib 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.
- vandetanib
vandetanib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- vemurafenib
vemurafenib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- voriconazole
voriconazole will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
voriconazole and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation. - vorinostat
vorinostat and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- voxelotor
voxelotor will increase the level or effect of glasdegib 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.
- ziprasidone
ziprasidone and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
Monitor Closely (21)
- albuterol
albuterol and glasdegib both increase QTc interval. Use Caution/Monitor.
- cenobamate
cenobamate will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.
- dengue vaccine
glasdegib decreases effects of dengue vaccine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Immunosuppressive therapies (eg, irradiation, antimetabolites, alkylating agents, cytotoxic drugs, corticosteroids [greater than physiologic doses]) may reduce immune response to dengue vaccine.
- deutetrabenazine
deutetrabenazine and glasdegib both increase QTc interval. Use Caution/Monitor. At the maximum recommended dose, deutetrabenazine does not prolong QT interval to a clinically relevant extent. Certain circumstances may increase risk of torsade de pointes and/or sudden death in association with drugs that prolong the QTc interval (eg, bradycardia, hypokalemia or hypomagnesemia, coadministration with other drugs that prolong QTc interval, presence of congenital QT prolongation).
- elagolix
elagolix decreases levels of glasdegib 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.
- fedratinib
fedratinib will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.
- fostemsavir
glasdegib and fostemsavir both increase QTc interval. Use Caution/Monitor. QTc prolongation reported with higher than recommended doses of fostemsavir.
- istradefylline
istradefylline will increase the level or effect of glasdegib 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.
- itraconazole
itraconazole will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Consider alternate therapies that are not strong CYP3A inhibitors or monitor for increased risk of adverse effects, including QTc interval prolongation.
- lenacapavir
lenacapavir will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lencapavir may increase CYP3A4 substrates initiated within 9 months after last SC dose of lenacapavir, which may increase potential risk of adverse reactions of CYP3A4 substrates.
- osilodrostat
osilodrostat and glasdegib both increase QTc interval. Use Caution/Monitor.
- ozanimod
ozanimod and glasdegib both increase QTc interval. Modify Therapy/Monitor Closely. The potential additive effects on heart rate, treatment with ozanimod should generally not be initiated in patients who are concurrently treated with QT prolonging drugs with known arrhythmogenic properties.
- ribociclib
ribociclib will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- rucaparib
rucaparib will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.
- selpercatinib
selpercatinib increases toxicity of glasdegib by QTc interval. Use Caution/Monitor.
- siponimod
siponimod and glasdegib 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.
- sodium sulfate/?magnesium sulfate/potassium chloride
sodium sulfate/?magnesium sulfate/potassium chloride increases toxicity of glasdegib by QTc interval. Use Caution/Monitor. Consider predose and post-colonoscopy ECGs in patients at increased risk of serious cardiac arrhythmias. .
- sodium sulfate/potassium sulfate/magnesium sulfate
sodium sulfate/potassium sulfate/magnesium sulfate increases toxicity of glasdegib by QTc interval. Use Caution/Monitor. Consider predose and post-colonoscopy ECGs in patients at increased risk of serious cardiac arrhythmias. .
- tazemetostat
tazemetostat will decrease the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- valbenazine
valbenazine and glasdegib both increase QTc interval. Use Caution/Monitor.
- voclosporin
voclosporin, glasdegib. Either increases effects of the other by QTc interval. Use Caution/Monitor.
Minor (4)
- acetazolamide
acetazolamide will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- anastrozole
anastrozole will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- cyclophosphamide
cyclophosphamide will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- larotrectinib
larotrectinib will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
Adverse Effects
>10% (All Grades Glasdegib with Cytarabine)
Increased creatinine (96%)
Hyponatremia (11-54%)
Anemia (43%)
Hemorrhage (36%)
Fatigue (36%)
Hypomagnesemia (33%)
Febrile neutropenia (31%)
Thrombocytopenia (30%)
Edema (30%)
Musculoskeletal pain (30%)
Nausea (29%)
Increased AST (28%)
Increased blood bilirubin (25%)
Increased ALT (24%)
Increased alkaline phosphatase (23%)
Mucositis (21%)
Decreased appetite (21%)
Dysgeusia (21%)
Constipation (20%)
Rash (20%)
Abdominal pain (19%)
Pneumonia (19%)
Renal insufficiency (19%)
Pyrexia (18%)
Diarrhea (18%)
Vomiting (18%)
Dizziness (18%)
Hyperkalemia (16%)
Increased CPK (16%)
Muscle spasm (15%)
Decreased platelet count (15%)
Hypokalemia (15%)
Weight decreased (13%)
Atrial arrhythmia (13%)
Chest pain (12%)
Headache (12%)
>10% (Glasdegib with Cytarabine Grade ≥3)
Anemia (41%)
Febrile neutropenia (31%)
Thrombocytopenia (30%)
Pneumonia (15%)
Decreased platelet count (15%)
Fatigue (14%)
Dyspnea (11%)
Decreased WBC count (11%)
1-10% (Glasdegib with Cytarabine Grade ≥3)
Hyponatremia (7%)
Hemorrhage (6%)
Hyponatremia (6%)
Renal insufficiency (5%)
Diarrhea (4%)
Atrial arrhythmia (4%)
Increased blood bilirubin (4%)
Musculoskeletal pain (2%)
Vomiting (2%)
Rash (2%)
Mucositis (1%)
Pyrexia (1%)
Chest pain (1%)
Nausea (1%)
Constipation (1%)
Decreased appetite (1%)
Increased creatinine (1%)
Increased AST (1%)
Hyperkalemia (1%)
1-10% (Glasdegib with Cytarabine)
<10%
- Dental disorders: Loose teeth, toothache
- Skin and subcutaneous tissue disorders: Alopecia
- Cardiac disorders: QT prolongation
Warnings
Black Box Warnings
Embryo-fetal toxicity
- Can cause embryo-fetal death or severe birth defects when administered to pregnant women; it is embryotoxic, fetotoxic, and teratogenic in animals
- Conduct pregnancy testing in females of reproductive potential before initiating
- Advise females of reproductive potential to use effective contraception during treatment and for at least 30 days after last dose
- Advise males of the potential risk of exposure through semen and to use condoms with a pregnant partner or a female partner of reproductive potential during treatment and for at least 30 days after last dose
Contraindications
None
Cautions
Based on mechanism of action and findings from animal studies, can cause embryo-fetal death or severe birth defects when administered to pregnant women (see Black Box Warnings and Pregnancy)
Development of QTc prolongation and ventricular arrhythmias reported, including ventricular fibrillation and ventricular tachycardia; more frequent ECG monitoring advised in patients with congenital long QT syndrome, congestive heart failure, electrolyte abnormalities, or those who are taking medications known to prolong the QTc interval (see Drug Interactions)
Drug interaction overview
- Glasdegib primarily metabolized by CYP3A
-
Strong CYP3A inhibitors
- Coadministration may increase glasdegib plasma concentrations and increase risk for QT prolongation
-
Strong or moderate CYP3A inducers
- Avoid; coadministration may decrease glasdegib plasma concentrations, thereby reducing efficacy
- May increase glasdegib dose if coadministration with moderate CYP3A4 inducers cannot be avoided
-
Prolonged QTc
- Associated with concentration-dependent QTc prolongation
- Avoid coadministration with QTc prolonging drugs
- If unavoidable, monitor for increased risk of QTc interval prolongation
Pregnancy
Pregnancy
Based on its mechanism of action and findings in animal embryo-fetal developmental toxicity studies, glasdegib can cause fetal harm when administered to pregnant women
Animal studies
- Exposure 3-4 times that of humans: Resulted in embryo-fetal lethality (eg, increased postimplantation loss and decreased numbers of live fetuses) in rats and rabbits
- Exposure 0.6 times that of humans: Fetal developmental abnormalities and malformations consisting of craniofacial malformations; malformed limbs, paws/digits, trunk, and tail; dilation of brain; malpositioned/malformed eyes; misshapen head; small tongue; absent palate, teeth, and viscera; diaphragmatic hernia; edema; heart defects; rib and vertebral abnormalities; malformed or absent structures in the appendicular skeleton
Infertility
- Males: Based on findings in repeat-dose animal toxicity studies in rats, may impair fertility in males of reproductive potential; some effects on male reproductive organs did not recover
Contraception
-
Females of reproductive potential
- Use effective contraception during treatment and for at least 30 days after last dose
- Do not donate blood during treatment and for at least 30 days after last dose
-
Males
- Unknown if present in semen
- Advise males of the potential risk of exposure through semen and to use effective contraception, including a condom, even after a vasectomy, to avoid drug exposure to a pregnant partner or a female partner of reproductive potential during treatment for at least 30 days after last dose
- Advise males to not donate sperm or blood during treatment and for at least 30 days after last dose
Lactation
- No data are available on the presence in human milk, effects on the breastfed child, or effect on milk production
- Advise women not to breastfeed or provide breast milk to infants or children during treatment and for at least 30 days after last dose
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
Inhibits the smoothen (SMO) receptor, a transmembrane protein involved in hedgehog (Hh) signal transduction, thereby disrupting the Hh pathway
SMO inhibition of Hh signaling impacts tumor biology by disrupting the regulation of cancer stem cell survival; this may inhibit development of drug resistance and prevent relapse
Absorption
Bioavailability: 77%
Peak plasma time: 1.3-1.8 hr
Peak plasma concentration: 1,252 ng/mL
AUC: 17,210 ng·hr/mL
Steady-state: Achieved by 8 days of daily dosing
Effect of food: High-fat, high-calorie meal reduced glasdegib’s AUC (16%) and peak plasma concentration (31%)
Distribution
Protein bound: 91%
Vd: 188 L
Metabolism
Primary metabolic pathway: CYP3A4
Minor metabolic pathways: CYP2C8 and UGT1A9
Elimination
Half-life: 17.4 hr
Clearance: 6.45 L/hr
Excretion: Urine (49% [17% unchanged]); feces (42%] 20% unchanged])
Administration
Oral Administration
Administer with or without food
Swallow tablet whole; do not split or crush
Administer at about the same time each day
Missed or vomited dose
- Vomited dose: Do not replace dose; wait until the next scheduled dose is due
- Missed dose or not taken at usual time: Administer dose as soon as possible and at least 12 hr before the next scheduled dose; return to normal schedule the following day
- Do not administer 2 doses within 12 hr
Storage
Store at 20-25°C (68-77°F); excursions permitted between 15-30°C (59-86°F)
Images
Formulary
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