Altretamine
Altretamine is an oral antineoplastic agent used primarily in the treatment of refractory ovarian cancer. It functions as a prodrug that is metabolized in the body to form reactive alkylating metabolites, which cross-link DNA strands and prevent cancer cell replication, leading to programmed cell death. This medication is typically reserved for patients who have not responded adequately to other chemotherapy regimens.
Altretamine is an oral chemotherapy agent used for refractory ovarian cancer that works by alkylating DNA to prevent cancer cell division.
Key facts at a glance
- ATC
- L01XX03
- RxNorm
- 5296
- Generic
- Altretamine
- Class
- atc-l01
- Brands
- —
- Availability
- rx
- Lactation
- unknown
- Routes
- oral
- Forms
- capsule
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Dosage and administration
- Usual dose
- 500mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 250mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 400mg daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
Overdose information
Special Populations
10 groupspregnancy
first trimesteravoid if possible
avoid use during pregnancy unless benefits outweigh risks - altretamine is an alkylating agent with potential teratogenic effects
regular fetal monitoring and ultrasound assessments
Use of this medication in this population requires careful consideration of risks and benefits.
pregnancy
second trimesteravoid if possible
avoid use during pregnancy unless benefits outweigh risks
regular fetal monitoring
Use of this medication in this population requires careful consideration of risks and benefits.
pregnancy
third trimesteravoid if possible
avoid use near term - consider delaying treatment until after delivery if possible
fetal monitoring and assessment of fetal growth
Use of this medication in this population requires careful consideration of risks and benefits.
lactation
breastfeedingdiscontinue breastfeeding
do not breastfeed during altretamine therapy and for at least 2 weeks after last dose
not applicable
Use of this medication in this population requires careful consideration of risks and benefits.
pediatric_age
children under 18use with caution - limited pediatric data available
use only in pediatric oncology settings with experience; dosing based on body surface area
close monitoring of hematologic parameters and organ function
Use with caution and monitor for adverse effects.
geriatric
elderly 65 plusno specific dose adjustment; start at lower end of dosing range
monitor renal and hepatic function; assess for comorbidities; increased risk of hematologic toxicity
more frequent blood count monitoring and organ function tests
Use with caution and monitor for adverse effects.
renal_impairment
mildno specific adjustment needed for mild impairment
monitor renal function; no initial dose reduction required
regular renal function monitoring
Use with caution and monitor for adverse effects.
renal_impairment
moderate to severereduce dose based on creatinine clearance
reduce initial dose; monitor closely; consider 25-50% dose reduction in severe impairment
frequent renal function monitoring and drug level monitoring if available
Use with caution and monitor for adverse effects.
hepatic_impairment
mildno specific adjustment for mild impairment
monitor hepatic function; no initial dose reduction required
regular liver function tests
Use with caution and monitor for adverse effects.
hepatic_impairment
moderate to severereduce dose; consider 25-50% dose reduction
use with extreme caution; monitor hepatic function closely; may require significant dose reduction
frequent liver function tests and clinical monitoring
Use with caution and monitor for adverse effects.
Statistics and clinical data
FDA approval year
FDA approved for ovarian cancer treatment
Drug class
Chemotherapeutic alkylating agent
Primary indication
Primary therapeutic use
Mechanism of action
DNA alkylation causing cross-linking
Primarily used for the treatment of refractory ovarian cancer in patients who have not responded to other chemotherapy agents. May also be investigated for use in other solid tumors in certain circumstances.
Altretamine is a prodrug that undergoes hepatic metabolism to form reactive alkylating intermediates. These metabolites cross-link DNA strands, disrupting DNA replication and transcription, ultimately inducing apoptosis in rapidly dividing cancer cells.
Administered orally in multiple daily doses. Requires regular monitoring of complete blood counts due to risk of bone marrow suppression. May cause neurotoxicity and gastrointestinal side effects. Contraindicated in patients with severe bone marrow suppression or known hypersensitivity. Pregnancy category D - contraindicated during pregnancy due to teratogenic potential.
Contraindications
Conditions and patient states where this medication should be avoided or used with caution.
Do not use (1)
Known allergy to this medication or its components
Use caution (1)
Consult healthcare provider for benefits vs risks assessment
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed August 24, 2026. · Read our editorial policy