Name: Altretamine

What should I do if I forget a dose?

Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

What side effects can this medication cause?

Altretamine may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

  • nausea
  • vomiting
  • loss of appetite
  • unusual tiredness or weakness
  • dizziness
  • pale skin
  • fainting
  • skin rash
  • itching
  • hair loss

Some side effects can be serious. If you experience any of these symptoms or those listed in the IMPORTANT WARNING section, call your doctor immediately or get emergency medical treatment:

  • fever, chills, sore throat, ongoing cough and congestion, or other signs of an infection
  • unusual bleeding or bruising
  • bloody or black, tarry stools
  • bloody vomit
  • vomited material that looks like coffee grounds
  • bleeding gums
  • small, round, red or purple colored spots on the skin

Altretamine may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.

If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting program online ( or by phone (1-800-332-1088).

Patient information

No information provided. Please refer to the WARNINGS and PRECAUTIONS sections.

Altretamine Brand Names

Altretamine may be found in some form under the following brand names:

  • Hexalen

Altretamine Drug Class

Altretamine is part of the drug class:


Inform MD

Before receiving altretamine, tell your doctor about all your medical conditions including if you:

  • are allergic to altretamine or any other medicine
  • have seizure disorders, nervous system disease, or blood disorders

Tell your doctor if you are pregnant or breastfeeding.

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements.

What is altretamine?

Altretamine is a cancer medicine that interferes with the growth and spread of cancer cells in the body.

Altretamine is used to ease the symptoms of ovarian cancer. This medication will not treat the cancer itself.

Altretamine is usually given after other cancer medicines have been tried without success.

Altretamine may also be used for purposes not listed in this medication guide.

What should I discuss with my healthcare provider before taking altretamine?

You should not use altretamine if you are allergic to it, or if you have:

  • severe nerve problems; or

  • severe bone marrow suppression.

To make sure altretamine is safe for you, tell your doctor if you have:

  • bone marrow problems;

  • any problems with your nervous system (brain or nerves); or

  • if you have recently used an MAO inhibitor--isocarboxazid, linezolid, methylene blue injection, phenelzine, rasagiline, selegiline, tranylcypromine, and others.

Do not use altretamine if you are pregnant. It could harm the unborn baby. Use effective birth control, and tell your doctor if you become pregnant during treatment.

It is not known whether altretamine passes into breast milk or if it could harm a nursing baby. You should not breast-feed while using this medicine.

How should I take altretamine?

Altretamine is usually taken 4 times per day. Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.

Altretamine is given in a 28-day treatment cycle, and you may only need to take the medicine during the first 2 or 3 weeks of each cycle. Your doctor will determine how long to treat you with altretamine.

Take altretamine after meals and at bedtime, unless your doctor tells you otherwise.

Altretamine can lower blood cells that help your body fight infections and help your blood to clot. Your blood will need to be tested often. Your cancer treatments may be delayed based on the results of these tests.

Your nerve and muscle function may also need to be checked.

Store at room temperature away from moisture and heat.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Altretamine side effects

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Stop using altretamine and call your doctor at once if you have:

  • severe numbness, tingling, or cold feeling in your hands or feet;

  • severe or continuous vomiting;

  • fever, chills, flu symptoms, mouth sores, pale skin, easy bruising or bleeding, unusual weakness;

  • a light-headed feeling, like you might pass out;

  • severe dizziness or spinning sensation;

  • seizure (convulsions); or

  • upper stomach pain, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).

Common side effects may include:

  • mild nausea or vomiting;

  • mild numbness or tingling;

  • loss of appetite;

  • mood changes, mild dizziness; or

  • skin rash, itching, hair loss.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

altretamine Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

Less common or rare
  • Black, tarry stools
  • blood in urine or stools
  • cough or hoarseness, accompanied by fever or chills
  • fever or chills
  • lower back or side pain, accompanied by fever or chills
  • painful or difficult urination, accompanied by fever or chills
  • pinpoint red spots on skin
  • unusual bleeding or bruising
  • unusual tiredness

Check with your doctor as soon as possible if any of the following side effects occur:

More common
  • Anxiety
  • clumsiness
  • confusion
  • convulsions (seizures)
  • dizziness
  • mental depression
  • numbness in arms or legs
  • weakness
  • Skin rash or itching

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common
  • Nausea and vomiting
Less common
  • Diarrhea
  • loss of appetite
  • stomach cramps

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Consumer Information Use and Disclaimer

  • If your symptoms or health problems do not get better or if they become worse, call your doctor.
  • Do not share your drugs with others and do not take anyone else's drugs.
  • Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
  • Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
  • Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about this medicine, please talk with your doctor, nurse, pharmacist, or other health care provider.
  • If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

This information should not be used to decide whether or not to take altretamine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to altretamine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.

Review Date: October 4, 2017

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule, Oral:

Hexalen: 50 mg

Brand Names U.S.

  • Hexalen

Pharmacologic Category

  • Antineoplastic Agent, Alkylating Agent


Altretamine structurally resembles alkylating agents, although has demonstrated activity in tumors resistant to classic alkylating agents. Cytotoxic effect not fully characterized, however it is likely that after activation, metabolites form crosslinks with DNA and RNA and inhibit DNA and RNA synthesis (Perry 2012). Altretamine has demonstrated more activity in platinum-sensitive ovarian cancers than platinum-resistant disease (Alberts 2004).


Well absorbed


Distributed into tissues high in lipid content and into tumor tissue (Damia 1995)


Hepatic; rapid and extensive demethylation to active metabolites (pentamethylmelamine and tetramethylmelamine)


Urine (90% [at 72 hours], <1% as unchanged drug)

Time to Peak

Plasma: 0.5 to 3 hours

Half-Life Elimination

4.7 to 10.2 hours

Dosing Hepatic Impairment

There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).

Dosing Obesity

ASCO Guidelines for appropriate chemotherapy dosing in obese adults with cancer: Utilize patient’s actual body weight (full weight) for calculation of body surface area- or weight-based dosing, particularly when the intent of therapy is curative; manage regimen-related toxicities in the same manner as for nonobese patients; if a dose reduction is utilized due to toxicity, consider resumption of full weight-based dosing with subsequent cycles, especially if cause of toxicity (eg, hepatic or renal impairment) is resolved (Griggs, 2012).

What should i discuss with my healthcare provider before taking altretamine (hexalen)?

Before taking altretamine, tell your doctor if you have:

  • any nervous system (brain and nerves) problems; or
  • bone marrow problems.

You may not be able to take altretamine, or you may require a dosage adjustment or special monitoring during treatment if you have any of the conditions listed above.

Altretamine is in the FDA pregnancy category D. This means that altretamine is known to cause birth defects in an unborn baby. Do not take altretamine without first talking to your doctor if you are pregnant or could become pregnant during treatment. Contraceptive measures are recommended during treatment with altretamine.

It is not known whether altretamine passes into breast milk. Do not take altretamine without first talking to your doctor if you are breast feeding a baby.

What happens if i miss a dose (hexalen)?

Contact your doctor if you miss a dose of altretamine.


-This drug should only be given under the supervision of a physician experienced in the use of antineoplastic agents.
-Peripheral blood counts should be monitored at least monthly, prior to the initiation of each treatment course and as clinical indicated.
-Neurological examination should be performed regularly during treatment because of the possibility of drug-related neurotoxicity.

Safety and efficacy have not been established in patients younger than 18 years.

Consult WARNINGS section for additional precautions.


Data not available