Dosing & Uses
Dosage Forms & Strengths
capsule
- 50mg
Recurrent Ovarian Cancer
Indicated for recurrence following alkylating agent or cisplatin treatment
260 mg/m²/day PO divided q6hr for 14-21 days of a 28-day cycle
Dosage Modifications
Renal or hepatic impairment: Dose adjustment not required
Temporarily hold and restart at 200 mg/m²/day if any of the following develop
- GI intolerance unresponsive to symptomatic treatment
- WBC <2000/mm³ or granulocytes <1000/mm³
- Platelets <75,000/mm³
- Progressive neurotoxicity
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (2)
- influenza virus vaccine quadrivalent, adjuvanted
altretamine 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.
- ropeginterferon alfa 2b
ropeginterferon alfa 2b, altretamine. Either increases toxicity of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Myelosuppressive agents can produce additive myelosuppression. Avoid use and monitor patients receiving the combination for effects of excessive myelosuppression.
Monitor Closely (3)
- isavuconazonium sulfate
altretamine and isavuconazonium sulfate both decrease immunosuppressive effects; risk of infection. Use Caution/Monitor.
- ofatumumab SC
ofatumumab SC, altretamine. 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.
- trastuzumab deruxtecan
trastuzumab deruxtecan, altretamine. 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. .
Minor (0)
Adverse Effects
>10%
Anemia (33%)
Nausea/vomiting (33%)
Peripheral sensory neuropathy (31%)
Thrombocytopenia (31%)
1-10%
Alk phos increased (9%)
Leukopenia (5%)
Anorexia (1%)
Seizures (1%)
<1%
Alopecia
Rash
Depression
Dizziness
Hepatotoxicity
Vertigo
Warnings
Black Box Warnings
Administer under the supervision of an experienced cancer chemotherapy physician
Bone marrow suppression
- Perform peripheral blood counts routinely before and after drug therapy
Neurotoxicity
- Perform neurologic examinations routinely before and after drug therapy
Contraindications
Hypersensitivity
Pre-existing severe bone marrow suppression or severe neurologic toxicity
Cautions
Neurotoxic-perform regular neurologic exams
Previous treatment with other myelosuppressive drugs or pre-existing neurotoxicity
Discontinue indefinitely if neurologic symptoms persist on reduced dose
Risk of orthostatic hypotension with concomitant MAO inhibitors, esp in >60 years
Avoid pregnancy
Pregnancy & Lactation
Pregnancy Category: D
Lactation: excretion in milk unknown/not recommended
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
Unclear, reactive intermediates covalently bind to microsomal proteins & DNA, possibly causing DNA damage
Metabolism required for cytotoxicity
Pharmacokinetics
Absorption: Well absorbed
Distribution: Highly concentrated in liver, kidney & small intestine
Protein Bound: Plasma proteins
Peak Plasma Time: 0.5-3 hr
Half-life: 7 hr
Metabolism: Liver; rapid & extensive demethylation to active metabolites
Excretion: Urine (90%; <1% as unchanged drug)
Administration
Oral Administration
Administer after meals and at bedtime
Monitor: Peripheral blood counts at least qMonth
