Altretamine: ovarian cancer use, dosing, and side effects
Last updated September 7, 2026.
Altretamine is a prescription oral chemotherapy capsule, sold as Hexalen, that is classified with the alkylating agents. Its exact mechanism is not fully known, but it damages the DNA of fast-dividing cancer cells so they stop multiplying. Because it also affects normal fast-growing cells and nerve tissue, it is given in cycles with blood counts and a neurologic check before each one. The single most important safety point is that you need regular monitoring: falling blood counts or spreading numbness and weakness are reasons to hold the drug, not to push through.
What does it treat?
Altretamine is approved as a single agent for persistent or recurrent ovarian cancer in people who have already been treated with first-line chemotherapy based on cisplatin, an alkylating agent, or both. In practice that means a cancer that came back or never fully responded after platinum-based treatment, and it is often chosen when someone wants an oral option instead of another intravenous regimen. It is not a first treatment for newly diagnosed ovarian cancer, and it is not used for other tumor types outside of research settings. There are no fixed-dose combination products that contain altretamine; it is taken on its own, though your oncologist may pair it with anti-nausea medicine and sometimes vitamin B6 for nerve symptoms.
How do you take it?
Altretamine comes as 50 mg capsules. The labeled dose is 260 mg per square meter of body surface area per day, which your oncology team calculates for you and splits into 4 doses: after breakfast, after lunch, after dinner, and at bedtime. It is given for either 14 or 21 days in a row within a 28-day cycle, then paused so your counts recover. Taking each dose right after food and at bedtime cuts down nausea, so do not take it on an empty stomach. If you miss a dose, skip it and take the next one at its usual time; never double up. If nausea and vomiting will not settle with your anti-nausea medicine, or you develop numbness, tingling, or weakness that is getting worse, stop the drug and call your oncology team the same day. Doses are also held for a white cell count under 2,000 per cubic millimeter, granulocytes under 1,000, or platelets under 75,000, and treatment is often restarted at 200 mg per square meter per day.
Side effects to know
- Common: Nausea and vomiting are the most common effects and tend to build over the first few weeks, and many people also have loss of appetite, fatigue, and mild tingling in the fingers or toes.
- Serious: Stop the capsules and get medical help the same day for a fever of 100.4 F or higher, chills, unusual bruising or bleeding, or black or bloody stools, which can mean your blood counts have dropped too low. Also stop and call for numbness, tingling, weakness, or unsteadiness that keeps spreading or makes it hard to walk, button a shirt, or hold a cup, since nerve damage can become permanent if the drug is continued.
Who should not take it?
Do not take altretamine if you already have severe bone marrow suppression or severe nerve damage from earlier treatment. Tell your doctor before starting if you have kidney or liver disease, an active infection, a history of neuropathy from platinum drugs or diabetes, or if you are getting other chemotherapy or radiation. Monoamine oxidase inhibitors such as phenelzine, tranylcypromine, selegiline, and linezolid can combine with altretamine to cause severe drops in blood pressure when you stand, and cimetidine slows the drug's clearance and raises toxicity, so both need to be reviewed and usually changed. Altretamine can harm a developing baby, so it is not used in pregnancy; people who can become pregnant should use effective birth control during treatment and confirm with their oncologist how long to continue it afterward, and partners should ask about contraception too. Breastfeeding is not recommended while taking it. There is no safe daily drinking level on this drug: alcohol worsens nausea, dizziness, and dehydration and adds strain to the liver, so plan to skip it while you are on a cycle.
When is it an emergency?
Call 911 for trouble breathing, swelling of the lips, face, or throat, hives with lightheadedness, fainting or collapse, seizures, or chest pain. If you or someone else takes too many capsules, call Poison Control at 1-800-222-1222 right away, even if there are no symptoms yet; an overdose mainly shows up as relentless vomiting, deep drowsiness or confusion, and rapidly worsening numbness or weakness, and the danger from very low blood counts can appear days later. Go to an emergency department the same day for a fever of 100.4 F or higher, shaking chills, bleeding that will not stop, vomiting blood or material that looks like coffee grounds, black tarry stools, or vomiting so persistent that you cannot keep fluids down.
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Common questions
What is the maximum dose of altretamine I can take in a day?
The labeled dose is 260 mg per square meter of body surface area per day, taken in 4 divided doses. For most adults that works out to roughly 400 to 500 mg total per day, but the exact number is calculated from your height and weight, so use the amount written on your prescription rather than a general figure. After a toxicity such as low blood counts or nerve symptoms, treatment is often restarted at the lower dose of 200 mg per square meter per day. Never add an extra capsule to make up for a missed dose or a vomited one without asking your oncology team first.
Can I drink alcohol while taking altretamine?
It is best to avoid alcohol during your treatment cycles. Altretamine already causes nausea and vomiting in most people, and alcohol makes that worse and increases the risk of dehydration. Alcohol also adds dizziness and unsteadiness on top of the nerve effects this drug can cause, which raises your chance of a fall. If you want to have a drink during a rest week between cycles, ask your oncologist first, since your liver function and blood counts factor into the answer.
Is altretamine safe during pregnancy or breastfeeding?
No. Altretamine can cause harm to a developing baby, and it is not used during pregnancy. If you can become pregnant, you will usually take a pregnancy test before starting and use effective contraception throughout treatment; ask your oncologist how long to keep using it after your last dose. If you become pregnant while taking it, stop and call your care team the same day. Breastfeeding is not recommended while you are on altretamine because the drug can pass into breast milk.
Do I have to take altretamine with food?
Yes. Each of the 4 daily doses is meant to be taken right after a meal, with the fourth dose at bedtime. Food significantly reduces the nausea that otherwise builds up over the first weeks of treatment. If you cannot eat a full meal, take the capsule with crackers, toast, or a nutrition drink rather than on an empty stomach. Anti-nausea medicine taken 30 to 60 minutes before your dose can also help, and your oncology team can prescribe one if you do not already have it.
What are the signs of an altretamine overdose?
Overdose usually shows up as severe and unstoppable vomiting, heavy drowsiness or confusion, and numbness or weakness that gets worse quickly. Dangerously low blood counts can follow several days later and show up as fever, chills, mouth sores, bruising, or bleeding. Call Poison Control at 1-800-222-1222 right away if too many capsules were taken, even if the person feels fine. Call 911 instead if the person collapses, has a seizure, or has trouble breathing. Bring the pill bottle with you so the team knows the exact dose.
Which medicines interact with altretamine?
Two interactions matter most. Monoamine oxidase inhibitors, including phenelzine, tranylcypromine, isocarboxazid, selegiline, and the antibiotic linezolid, can combine with altretamine to cause severe drops in blood pressure when you stand up, with fainting. Cimetidine slows how fast your body clears altretamine and increases its toxicity, so a different acid reducer is usually chosen. Other chemotherapy, radiation, and drugs that lower blood counts add to bone marrow suppression. Give your oncology team a full list including over-the-counter products and supplements before each cycle.