Dosing & Uses
Dosage Forms & Strengths
powder for injection
- 4mg/vial
capsule
- 0.25mg
- 1mg
Small Cell Lung Cancer
Indicated for SCLC sensitive disease after failure of first-line chemotherapy
IV Infusion
Capsules
Cervical Cancer
Indicated for combination therapy with cisplatin for stage IV-B, recurrent or persistent cervical carcinoma which cannot be treated with surgery and/or radiation therapy
0.75 mg/m² IV infused over 30 min on Days 1,2, & 3 (with cisplatin 50 mg/m² on Day 1); repeat at 21-day cycles
Ovarian Cancer
Indicated for metastatic ovarian cancer after failure of initial or subsequent chemotherapy
1.5mg/m² IV qDay x5 days; repeat at 21-day cycles
Dosage Modifications
Renal impairment
IV infusion (monotherapy)
- Mild (CrCl 40-60 mL/min): No dosage adjustment necessary
- Moderate (CrCl 20-39 mL/min): Decrease dose to 0.75 mg/m² PO qDay
- Severe (CrCl <20 mL/min): Safety and efficacy has not been established
Capsules
- CrCl 30-49 mL/min: Decrease dose to 1.5 mg/m² PO day
- CrCl <30 mL/min: 0.6 mg/m² PO Day
- Dose may be increased after first course by 0.4 mg/m²/day if no severe hematologic or gastrointestinal toxicities occur
Hematologic toxicities
- Do not administer subsequent courses of until neutrophils recover to >1,000 cells/mm³, platelets recover to >100,000 cells/mm³, hemoglobin levels recover to ≥9.0 g/dL (with transfusion if necessary)
IV infusion (monotherapy)
- Neutrophil count <500 cells/mm³: Reduce dose to 1.25 mg/m² alternatively, granulocyte-colony stimulating factor (G-CSF) starting no sooner than 24 hours after topotecan administration has been completed
- Platelet count < 25.000 cells/mm³ during previous cycle: Reduce dose to 1.25 mg/m²
Combination therapy with cisplatin
- Severe neutropenia (neutrophil counts <1,000 cells/mm³ with temperature of ≥38.0°C (100.4°F)): Reduce dose to 0.60 mg/m² (and further to 0.45 mg/m² if necessary); alternatively, G-CSF starting no sooner than 24 hours after topotecan administration has been completed
- Platelet count <25.000 cells/mm³: Reduce dose to 0.60 mg/m² (and further to 0.45 mg/m² if necessary)
Diarrhea (capsules only)
- Do not administer to patients with Grade 3 or 4 diarrhea
- After recovery to ≤Grade 1, reduce the dose by 0.4 mg/m²/day PO for subsequent courses
Dosing Considerations
Verify dose using body surface area prior to dispensing
Recommended dosage should generally not exceed 4 mg IV
Prior to administration of the first treatment course, baseline counts for neutrophils should be >1,500/mm³ and platelets >100,000/mm³
Monitor: CBC
Safety and effectiveness not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (54)
- abiraterone
abiraterone will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- adenovirus types 4 and 7 live, oral
topotecan decreases effects of adenovirus types 4 and 7 live, oral by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Immunosuppressives may diminish therapeutic effects of vaccines and increase risk of adverse effects (increased risk of infection). Live-attenuated vaccines should be avoided for at least 3mo after cessation of immunosuppressive therapy.
- amiodarone
amiodarone will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- atorvastatin
atorvastatin will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- azithromycin
azithromycin will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- bremelanotide
bremelanotide will decrease the level or effect of topotecan by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- captopril
captopril will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- carvedilol
carvedilol will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- clarithromycin
clarithromycin will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- cobicistat
cobicistat will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- conivaptan
conivaptan will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- crizotinib
crizotinib will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- cyclosporine
cyclosporine will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance. Additionally, topotecan is a substrate of the BCRP efflux transporter. Cylcosporine also inhibits BCRP.
- darolutamide
darolutamide will increase the level or effect of topotecan by Other (see comment). Avoid or Use Alternate Drug. Darolutamide is a BCRP inhibitor. Avoid coadministration with BCRP inhibitors. If use is unavoidable, closely monitor for adverse reactions and consider dose reduction of BCRP substrate drug (refer BCRP substrate prescribing information).
- darunavir
darunavir will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- deferiprone
deferiprone, topotecan. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid use of deferiprone with other drugs known to be associated with neutropenia or agranulocytosis; if an alternative is not possible, monitor absolute neutrophil count more frequently.
- dipyridamole
dipyridamole will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- dronedarone
dronedarone will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- erythromycin base
erythromycin base will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- erythromycin ethylsuccinate
erythromycin ethylsuccinate will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- erythromycin lactobionate
erythromycin lactobionate will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- erythromycin stearate
erythromycin stearate will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- felodipine
felodipine will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- influenza virus vaccine quadrivalent, adjuvanted
topotecan decreases effects of influenza virus vaccine quadrivalent, adjuvanted by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Immunosuppressive drugs may reduce the immune response to influenza vaccine.
- influenza virus vaccine trivalent, adjuvanted
topotecan decreases effects of influenza virus vaccine trivalent, adjuvanted by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Immunosuppressive drugs may reduce the immune response to influenza vaccine.
- itraconazole
itraconazole will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- ketoconazole
ketoconazole will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- lapatinib
lapatinib will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- lasmiditan
lasmiditan increases levels of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.
lasmiditan increases levels of topotecan by Other (see comment). Avoid or Use Alternate Drug. Comment: Lasmiditan inhibits BCRP in vitro. Avoid coadministration of lasmiditan with BCRP substrates. - ledipasvir/sofosbuvir
ledipasvir/sofosbuvir will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- lomitapide
lomitapide will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- lopinavir
lopinavir will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- mefloquine
mefloquine increases levels of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.
- nelfinavir
nelfinavir will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- nicardipine
nicardipine will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- nilotinib
nilotinib will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- palifermin
palifermin increases toxicity of topotecan by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hrbefore, 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.
- quercetin
quercetin will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- quinidine
quinidine will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- quinine
quinine will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- ranolazine
ranolazine will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- ritonavir
ritonavir will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- saquinavir
saquinavir will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- sofosbuvir/velpatasvir
sofosbuvir/velpatasvir will increase the level or effect of topotecan by Other (see comment). Avoid or Use Alternate Drug. Velpatasvir is an inhibitor of the drug transporter BCRP. Coadministration may increase systemic exposure of drugs that are BCRP substrates.
- sotorasib
sotorasib will decrease the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If use is unavoidable, refer to the prescribing information of the P-gp substrate for dosage modifications.
- tacrolimus
tacrolimus will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- tamoxifen
tamoxifen will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- tepotinib
tepotinib will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If concomitant use unavoidable, reduce the P-gp substrate dosage if recommended in its approved product labeling.
- ticagrelor
ticagrelor will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- tolvaptan
tolvaptan will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- trilaciclib
trilaciclib will decrease the level or effect of topotecan by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- vandetanib
vandetanib will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- vemurafenib
vemurafenib will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- verapamil
verapamil will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
Monitor Closely (41)
- acalabrutinib
acalabrutinib increases levels of topotecan by Other (see comment). Use Caution/Monitor. Comment: Acalabrutinib may increase exposure to coadministered BCRP substrates by inhibition of intestinal BCRP.
acalabrutinib, topotecan. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration may increase risk of myelosuppressive effects. - apalutamide
apalutamide will decrease the level or effect of topotecan by increasing elimination. Use Caution/Monitor. Apalutamide weakly induces BCRP and may decrease systemic exposure of drugs that are BCRP substrates.
- belatacept
belatacept and topotecan both increase immunosuppressive effects; risk of infection. Use Caution/Monitor.
- berotralstat
berotralstat will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor or titrate P-gp substrate dose if coadministered.
- cholera vaccine
topotecan decreases effects of cholera vaccine by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Immunosuppressive therapies, including irradiation, antimetabolites, alkylating agents, cytotoxic drugs and corticosteroids (used in greater than physiologic doses), may reduce the immune response to cholera vaccine.
- cisplatin
topotecan, cisplatin. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Use alternatives if available. Additive myelosuppression.
- dengue vaccine
topotecan 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.
- denosumab
topotecan, denosumab. Other (see comment). Use Caution/Monitor. Comment: Caution should be taken in patients on concomitant immunosuppressants or with impaired immune systems because of increased risk for serious infections.
- elagolix
elagolix will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- eliglustat
eliglustat increases levels of topotecan by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Monitor therapeutic drug concentrations, as indicated, or consider reducing the dosage of the P-gp substrate and titrate to clinical effect.
- eltrombopag
eltrombopag will increase the level or effect of topotecan by Other (see comment). Use Caution/Monitor. Avoid coadministration. Topotecan is a substrate of the efflux transporter BCRP. Eltrombopag inhibits BCRP.
- eluxadoline
eluxadoline increases levels of topotecan by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered BCRP substrates. .
- ferric maltol
ferric maltol, topotecan. Either increases levels of the other by unspecified interaction mechanism. Modify Therapy/Monitor Closely. Coadministration of ferric maltol with certain oral medications may decrease the bioavailability of either ferric maltol and some oral drugs. For oral drugs where reductions in bioavailability may cause clinically significant effects on its safety or efficacy, separate administration of ferric maltol from these drugs. Duration of separation may depend on the absorption of the medication concomitantly administered (eg, time to peak concentration, whether the drug is an immediate or extended release product).
- fingolimod
topotecan increases effects of fingolimod by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Concomitant therapy is expected to increase the risk of immunosuppression. Use caution when switching patients from long-acting therapies with immune effects. .
- fostamatinib
fostamatinib will increase the level or effect of topotecan by decreasing metabolism. Use Caution/Monitor. Concomitant use of fostamatinib may increase concentrations of BCRP substrate drugs. Monitor for toxicities of BCRP substrate drug that may require dosage reduction when given concurrently with fostamatinib.
fostamatinib will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Concomitant use of fostamatinib may increase concentrations of P-gp substrates. Monitor for toxicities of the P-gp substrate drug that may require dosage reduction when given concurrently with fostamatinib. - fostemsavir
fostemsavir will increase the level or effect of topotecan by Other (see comment). Modify Therapy/Monitor Closely. Fostemsavir inhibits BCRP transporters. If possible, avoid coadministration or modify dose of BCRP substrate coadministered with fostemsavir.
- glecaprevir/pibrentasvir
glecaprevir/pibrentasvir will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of topotecan by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates. - hydroxyurea
topotecan, hydroxyurea. Other (see comment). Use Caution/Monitor. Comment: Combination may increase risk of myelosuppression.
- ifosfamide
ifosfamide, topotecan. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration with ifosfamide may increase the risk of immunosuppression and myelosuppression.
- istradefylline
istradefylline will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of P-gp substrates in clinical trials. Consider dose reduction of sensitive P-gp substrates.
- ivacaftor
ivacaftor increases levels of topotecan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Ivacaftor and its M1 metabolite has the potential to inhibit P-gp; may significantly increase systemic exposure to sensitive P-gp substrates with a narrow therapeutic index.
- lonafarnib
lonafarnib will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Lonafarnib is a weak P-gp inhibitor. Monitor for adverse reactions if coadministered with P-gp substrates where minimal concentration changes may lead to serious or life-threatening toxicities. Reduce P-gp substrate dose if needed.
- meningococcal group B vaccine
topotecan decreases effects of meningococcal group B vaccine by pharmacodynamic antagonism. Use Caution/Monitor. Individuals with altered immunocompetence may have reduced immune responses to the vaccine.
- ofatumumab SC
ofatumumab SC, topotecan. Either increases effects of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Consider the risk of additive immune system effects when coadministering immunosuppressive therapies with coadministration. When switching from therapies with immune effects, take into account the duration and mechanism of action of these therapies when initiating ofatumumab SC.
- olaparib
topotecan and olaparib both increase pharmacodynamic synergism. Use Caution/Monitor. Coadministration with other other myelosuppressive anticancer agents, including DNA damaging agents, may potentiate and prolongate the myelosuppressive toxicity.
- osimertinib
osimertinib will increase the level or effect of topotecan by Other (see comment). Modify Therapy/Monitor Closely. Osimertinib is an inhibitor of BCRP transport. Caution if coadministered with sensitive BCRP substrates.
- oxaliplatin
oxaliplatin, topotecan. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Closely monitor for hematologic toxicity (eg, neutropenia, thrombocytopenia). Interaction may be sequence dependent and primarily associated with regimens in which oxaliplatin is administered prior to topotecan. Lower doses are recommended when using this combination (in the sequence of platinum derivative prior to topotecan). Alternatively, consider using a sequence in which the platinum derivative is given after topotecan when possible.
- ponatinib
ponatinib increases levels of topotecan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
ponatinib increases levels of topotecan by Other (see comment). Use Caution/Monitor. - regorafenib
regorafenib will increase the level or effect of topotecan by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.
- rolapitant
rolapitant will increase the level or effect of topotecan by Other (see comment). Use Caution/Monitor. Oral rolapitant (BCRP inhibitor) may increase plasma concentrations of BCRP substrates and may result in potential adverse reactions. Monitor possible adverse reactions if concomitant use of BCRP substrates and rolapitant can not be avoided.
- safinamide
safinamide will increase the level or effect of topotecan by Other (see comment). Use Caution/Monitor. Safinamide and its major metabolite may inhibit intestinal BCRP. Monitor BCRP substrates for increased pharmacologic or adverse effects.
- sarecycline
sarecycline will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor for toxicities of P-gp substrates that may require dosage reduction when coadministered with P-gp inhibitors.
- siponimod
siponimod and topotecan 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.
- sipuleucel-T
topotecan decreases effects of sipuleucel-T by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.
- stiripentol
stiripentol will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Consider reducing the dose of P-glycoprotein (P-gp) substrates, if adverse reactions are experienced when administered concomitantly with stiripentol.
stiripentol will increase the level or effect of topotecan by Other (see comment). Use Caution/Monitor. Stiripentol is a CYP2C8 and BCRP transport inhibitor. Consider dosage reduction for BCRP substrates if adverse effects are experienced when coadministered. - tafamidis
tafamidis will increase the level or effect of topotecan by Other (see comment). Use Caution/Monitor. Tafamidis inhibits breast cancer resistant protein (BCRP) in vitro and may increase exposure of BCRP substrates following tafamidis or tafamidis meglumine administration. Dosage adjustment of these BCRP substrates may be necessary.
- tafamidis meglumine
tafamidis meglumine will increase the level or effect of topotecan by Other (see comment). Use Caution/Monitor. Tafamidis inhibits breast cancer resistant protein (BCRP) in vitro and may increase exposure of BCRP substrates following tafamidis or tafamidis meglumine administration. Dosage adjustment of these BCRP substrates may be necessary.
- trastuzumab
trastuzumab, topotecan. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .
- trastuzumab deruxtecan
trastuzumab deruxtecan, topotecan. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .
- tucatinib
tucatinib will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Consider reducing the dosage of P-gp substrates, where minimal concentration changes may lead to serious or life-threatening toxicities.
- ustekinumab
ustekinumab, topotecan. Other (see comment). Use Caution/Monitor. Comment: Formation of CYP450 enzymes can be altered by increased levels of certain cytokines during chronic inflammation; thus, normalizing the formation of CYP450 enzymes. Upon initiation or discontinuation of ustekinumab in patients who are receiving concomitant CYP450 substrates, particularly those with a narrow therapeutic index, consider monitoring for therapeutic effect.
Minor (2)
- vitamin A
vitamin A, topotecan. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Antioxidants such as vitamin A enhance the efficacy, and reduce toxicity, of antineoplastic drugs.
- vitamin E
vitamin E, topotecan. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Antioxidants such as vitamin E enhance the efficacy, and reduce toxicity, of antineoplastic drugs.
Adverse Effects
>10%
IV infusion
Ovarian cancer
- Neutropenia, grade 4 (80%)
- Anemia, grade 3 or 4 (41%)
- Thrombocytopenia, grade 4 (27%)
- Febrile neutropenia (23%)
Small cell lung cancer
- Neutropenia, grade 4 (70%)
- Anemia, grade 3 or 4 (42%)
- Thrombocytopenia. grade 4 (29%)
Cervical cancer (Combination therapy with cisplatin)
- Constitutional, grade 3 or 4 (69%)
- Pain, grade 3 or 4 (59%)
- Neutropenia, grade 4 (48%)
- Vomiting, grade 3 or 4 (40%)
- Anemia, grade 3 (34%)
- Thrombocytopenia, grade 3 (26%)
- Neutropenia, grade 3 (26%)
Capsule
All grades
- Anemia (98%)
- Sepsis (43%)
- Nausea (33%)
- Thrombocytopenia (29%)
- Neutropenia (24%)
Grade 3 or 4
- Neutropenia (24-32%)
- Thrombocytopenia (6-29%)
- Anemia (7-18%)
1-10%
IV infusion
Ovarian cancer
- Nausea, grade 3 or 4 (10%)
- Vomiting, grade 3 or 4 (10%)
- Fatigue, grade 3 or 4 (7%)
- Dyspnea, grade 3 or 4 (6%)
- Diarrhea, grade 3 or 4 (6%)
- Sepsis, grade 3 or 4 (5%)
- Abdominal pain, grade 3 or 4 (5%)
- Constipation, grade 3 or 4 (5%)
- Intestinal obstruction, grade 3 or 4 (5%)
- Asthenia, grade 3 or 4 (5%)
- Pain, grade 3 or 4 (5%)
Small cell lung cancer
- Neutropenia, grade 4 (9%)
- Asthenia, grade 3 or 4 (9%)
- Pneumonia, grade 3 or 4 (8%)
- Nausea, grade 3 or 4 (8%)
- Abdominal pain, grade 3 or 4 (6%)
- Fatigue, grade 3 or 4 (6%)
- Sepsis, grade 3 or 4 (5%)
Cervical cancer (Combination therapy with cisplatin)
- Thrombocytopenia, grade 4 (7%)
- Stomatitis-pharyngitis, grade 3 or 4 (6%)
Capsule
All grades
- Pyrexia (5%)
- Asthenia (7%)
Grade 3 or 4
- Diarrhea (4%)
- Fatigue (4%)
- Nausea (3%)
- Vomiting (3%)
- Anorexia (2%)
- Asthenia (2%)
- Pyrexia (1%)
<1%
Oral
- Diarrhea, grade 4 (0.4%)
- Vomiting, grade 4 (0.4%)
- Fatigue, grade 4 (0.1%)
- Alopecia, grade 3 (0.1%)
Postmarketing Reports
Blood and lymphatic system disorders: Myelosuppression, severe bleeding (in association with thrombocytopenia
Immune system disorders: Allergic manifestations, anaphylactoid reactions
Gastrointestinal Disorders: Gastrointestinal perforation; mucosal inflammation, abdominal pain potentially associated with neutropenic enterocolitis
Pulmonary disorders: Interstitial lung disease
Skin and subcutaneous tissue disorders: Angioedema, severe dermatitis, severe pruritus
General disorders and administration site conditions: Extravasation
Hepatobiliary disorders: Grade 1 transient elevations in hepatic enzymes (8%); Grade 3/4 (4%); Grade 3/4 elevated bilirubin (<2%)
Warnings
Black Box Warnings
Administer only to patients with baseline neutrophil counts of 1500 cells/mm³or higher and a platelet count of 100,000 cells/mm³ or higher; monitor blood cell counts
To assess the occurrence of bone marrow suppression, blood cell counts should be monitored
Contraindications
Hypersensitivity reactions to drug or any components
Cautions
Administer to patients with bone marrow suppression only if patient has adequate bone marrow reserves; monitor peripheral blood counts and adjust dose as needed
PO: Do NOT redose if ANC <1500/mm³; Plt 100,000 Avoid use in pregnancy; can cause fetal harm; advise women of potential risk to fetus Neutropenia: pancytopenia has been reported Grade 4 thrombocytopenia and grade 3-4 anemia reported; withhold and reduce dose based on neutrophil counts, platelet counts and hemoglobin levels Fatal cases of interstitial lung disease have occurred; permanently discontinue for confirmed ILD If extravasation occurs, immediately stop administration and institute recommended management procedures; severe cases reported PO: If patient vomits after taking capsule, do NOT repeat dose PO: If diarrhea occurs, treat aggressively, potentially life-threatening Monitor patients presenting with neutropenia, fever and abdominal pain; fatal typhlitis reported in patients with neutropenic enterocolitisas Monitor patients presenting with cough, fever, dyspnea and/or hypoxia and a history of lung disease as fatalities due to interstitial lung disease have been reportedCombination with cisplatin
Pregnancy & Lactation
Pregnancy
Based on animal data and its mechanism of action, therapy can cause fetal harm when administered to a pregnant woman; there are no available clinical data on use of therapy in pregnancy; drug caused embryolethality, fetotoxicity, and teratogenicity in rats and rabbits when administered during organogenesis at doses similar to the clinical dose.); advise pregnant women of potential risk to fetus
Verify pregnancy status of females of reproductive potential prior to initiating therapy
Contraception
- Advise females of reproductive potential to use effective contraception during treatment and for 6 months after last dose
Infertility
- Females: Therapy can have both acute and long-term effects on fertility
- Males: Effects on spermatogenesis occurred in animals administered topotecan; therapy may damage spermatozoa, resulting in possible genetic and fetal abnormalities; advise males with a female partner of reproductive potential to use effective contraception during treatment and for 3 months after the last dose
Lactation
There are no data on presence of drug or its metabolites in human milk or their effects on breastfed infant or on milk production; lactating rats excrete high concentrations of drug in milk
Because of potential for serious adverse reactions in breastfed infants, advise women not to breastfeed during treatment and for 1 week 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
Binds to topoisomerase I to produce double-strand breaks in DNA
Absorption
Bioavailability: 40% (PO)
Peak plasma time: 1-2 hr (PO)
Distribution
Protein Bound: 35%
Metabolism
Hepatic
Excretion
Half-life, terminal: 2-3 hr (IV); 3-6 hr (PO)
Excretion, PO: 35% feces; 22% urine
Excretion, IV: 20% feces; 54% urine
Administration
IV Incompatibilities
Y-site: dexamethasone sodium phosphate, fluorouracil, mitomycin, ticarcillin-clavulanate(?)
IV Compatibilities
Solution: D5W, NS
Y-site: carbopolatin, cisplatin, cimetidine, cyclophosphamide, doxorubicin, etoposide, gemcitabine, granisetron, ifosfamide, methylprednisolone Na-succinate, metoclopramide, ondansetro, paclitaxel, prochlorperazine, vincristine
IV Preparation
No preservatives-reconstitute immediately prior to use
Reconstitute in 4 mL SWI to obtain a 1 mg/mL solution
No preservatives-use immediately
Dilute in 50-250 mL NS or D5W; stability is pH dependent although topotecan may be further diluted in NS
IV Administration
Infuse over 30 min
Storage
Injection
- Unopened vials: Store at 20-25°C (68-77°F); protect from light in original carton; vials contain no preservative, contents should be used immediately after reconstitution
- Reconstituted vials: Store at 20-25°C (68-77°F) and ambient lighting conditions for 24 hr
- Diluted solutions: Store at 20-25°C (68-77°F) for ≤4 hr or under refrigerated at 2-8°C (36-46°F) for ≤12 hr
Capsule
- Store refrigerated 2-8ºC (36-46ºF); store bottles protected from light in original outer cartons
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Hycamtin oral - | 1 mg capsule |  | |
| Hycamtin oral - | 0.25 mg capsule |  | |
| topotecan intravenous - | 4 mg/4 mL (1 mg/mL) vial |  | |
| topotecan intravenous - | 4 mg/4 mL (1 mg/mL) vial |  | |
| topotecan intravenous - | 4 mg vial |  | |
| topotecan intravenous - | 4 mg vial |  | |
| topotecan intravenous - | 4 mg vial |  | |
| topotecan intravenous - | 4 mg vial |  | |
| topotecan intravenous - | 4 mg/4 mL (1 mg/mL) vial |  | |
| topotecan intravenous - | 4 mg/4 mL (1 mg/mL) vial |  | |
| topotecan intravenous - | 4 mg vial |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
topotecan intravenous
TOPOTECAN - INJECTION
(TOE-poe-TEE-kan)
COMMON BRAND NAME(S): Hycamtin
WARNING: Topotecan decreases bone marrow function, an effect that may lead to a low number of blood cells such as red cells, white cells, and platelets. This effect can cause anemia, decrease your body's ability to fight an infection, or cause easy bruising/bleeding. Tell your doctor right away if you develop any of the following symptoms: unusual tiredness, pale skin, signs of infection (such as sore throat that doesn't go away, fever, chills), easy bruising/bleeding.Your doctor will order blood tests to monitor your bone marrow function while you are using this medication. Keep all medical and lab appointments.
USES: This medication is used to treat ovarian, lung, or cervical cancer. It is a chemotherapy drug that works by slowing or stopping the growth of cancer cells.
HOW TO USE: This medication is given by a health care professional. It is injected slowly into a vein over 30 minutes. The dosage is based on your medical condition, body size, laboratory tests, and response to treatment.
SIDE EFFECTS: See also Warning section.Nausea, vomiting, constipation, diarrhea, abdominal pain, weakness, tiredness, or mouth sores may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.People using this medication may have serious side effects. However, you have been prescribed this drug because your doctor has judged that the benefit to you is greater than the risk of side effects. Careful monitoring by your doctor may decrease your risk.Tell your doctor right away if you have any serious side effects, including: pain/redness/bruising at injection site, signs of lung problems (such as cough, shortness of breath).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: Before using topotecan, 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: kidney disease.This drug may make you feel weak or tired. Alcohol or marijuana (cannabis) can make you more tired. 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).Topotecan 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.Do not have immunizations/vaccinations without the consent of your doctor. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).To lower the chance of getting cut, bruised or injured, use caution with sharp objects like razors and nail cutters, and avoid activities such as contact sports.This medication can affect fertility in both males and females. Ask your doctor for more details.Tell your doctor if you are pregnant or plan to become pregnant. You should not become pregnant while using topotecan. Topotecan may harm an unborn baby. Ask your doctor about reliable forms of birth control. Females should use birth control during treatment and for 6 months after stopping this drug. Males should use birth control during treatment and for 3 months after stopping this drug. If you or your partner become pregnant, talk to your 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 drug and for 1 week after stopping this drug. 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.
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.
NOTES: Lab and/or medical tests (such as complete blood count, kidney/liver function) should be done while you are using this medication. Keep all medical and lab appointments. Consult your doctor for more details.
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.
STORAGE: Not applicable. This medication is given in a clinic and will not be stored at home.
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 August 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.
