Pralatrexate

What is pralatrexate used for?

Pralatrexate is a prescription medicine that is used to treat a type of lymphoma. Pralatrexate may be given to you for other reasons.

Description

Pralatrexate is a dihydrofolate reductase inhibitor. Pralatrexate has the chemical name (2S)-2-[[4-[(1RS)-1-[(2, 4-diaminopteridin-6-yl)methyl]but-3- ynyl]benzoyl]amino]pentanedioic acid. The molecular formula is C23H23N7O5 and the molecular weight is 477.48 g/mol. Pralatrexate is a 1:1 racemic mixture of S- and R- diastereomers at the C10 position (indicated with *). The structural formula is as follows:

Pralatrexate is an off-white to yellow solid. It is soluble in aqueous solutions at pH 6.5 or higher. Pralatrexate is practically insoluble in chloroform and ethanol. The pKa values are 3.25, 4.76, and 6.17.

FOLOTYN (pralatrexate) is supplied as a preservative-free, sterile, isotonic, non-pyrogenic clear yellow aqueous solution contained in a clear glass single-dose vial (Type I) for intravenous use. Each 1 mL of solution contains 20 mg of pralatrexate, sufficient sodium chloride to achieve an isotonic (280-300 mOsm) solution, and sufficient sodium hydroxide, and hydrochloric acid if needed, to adjust and maintain the pH at 7.5-8.5. FOLOTYN is supplied as either 20 mg (1 mL) or 40 mg (2 mL) single-dose vials at a concentration of 20 mg/mL.

Mechanism of Action

Pralatrexate is a folate analog metabolic inhibitor that competitively inhibits dihydrofolate reductase. It is also a competitive inhibitor for polyglutamylation by the enzyme folylpolyglutamyl synthetase. This inhibition results in the depletion of thymidine and other biological molecules the synthesis of which depends on single carbon transfer.

Before taking pralatrexate, tell your doctor:

• If you are allergic to pralatrexate; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.
• If you have kidney disease.

This is not a list of all drugs or health problems that interact with pralatrexate.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take pralatrexate with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take pralatrexate?

• Tell all of your health care providers that you take pralatrexate. This includes your doctors, nurses, pharmacists, and dentists.
• Have blood work checked as you have been told by the doctor. Talk with the doctor.
• You may have more chance of getting an infection. Wash hands often. Stay away from people with infections, colds, or flu.
• You may bleed more easily. Be careful and avoid injury. Use a soft toothbrush and an electric razor.
• If you have upset stomach, throwing up, diarrhea, or are not hungry, talk with your doctor. There may be ways to lower these side effects.
• Mouth irritation and mouth sores are common with pralatrexate. These side effects may happen as early as a few days after getting pralatrexate. Do what your doctor or other health care provider tells you to prevent mouth irritation or mouth sores. Call your doctor if mouth irritation or mouth sores get very bad, bother you, or do not go away.
• Patients with cancer who take pralatrexate may be at a greater risk of getting a severe health problem called tumor lysis syndrome (TLS).This may lead to death. Call your doctor right away if you have a fast or abnormal heartbeat; any passing out; trouble passing urine; muscle weakness or cramps; upset stomach, throwing up, diarrhea, or not able to eat; or feel sluggish.
• If you are 65 or older, use pralatrexate with care. You could have more side effects.
• This medicine may cause harm to an unborn baby. Women must use birth control while taking pralatrexate. If you get pregnant, call your doctor right away.
• Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

How is pralatrexate best taken?

Use pralatrexate as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• It is given into a vein for a period of time.
• You will need to have vitamin B12 shots before your first dose and while you are using pralatrexate. Talk with your doctor.
• Take folic acid as your doctor tells you before, during, and after using pralatrexate. Talk with your doctor.

What do I do if I miss a dose?

• Call your doctor to find out what to do.

What are the side effects of pralatrexate that I need to call my doctor about immediately?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Signs of infection like fever, chills, very bad sore throat, ear or sinus pain, cough, more sputum or change in color of sputum, pain with passing urine, mouth sores, or wound that will not heal.
• Signs of bleeding like throwing up or coughing up blood; vomit that looks like coffee grounds; blood in the urine; black, red, or tarry stools; bleeding from the gums; abnormal vaginal bleeding; bruises without a cause or that get bigger; or bleeding you cannot stop.
• Signs of liver problems like dark urine, feeling tired, not hungry, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes.
• Signs of fluid and electrolyte problems like mood changes, confusion, muscle pain or weakness, a heartbeat that does not feel normal, very bad dizziness or passing out, fast heartbeat, more thirst, seizures, feeling very tired or weak, not hungry, unable to pass urine or change in the amount of urine produced, dry mouth, dry eyes, or very bad upset stomach or throwing up.
• Shortness of breath.
• Pale skin.
• Swelling.
• A very bad skin reaction (toxic epidermal necrolysis) may happen. It can cause very bad health problems that may not go away, and sometimes death. Get medical help right away if you have signs like red, swollen, blistered, or peeling skin (with or without fever); red or irritated eyes; or sores in your mouth, throat, nose, or eyes.

What are some other side effects of pralatrexate?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Feeling tired or weak.
• Constipation, diarrhea, stomach pain, upset stomach, throwing up, or feeling less hungry.
• Sore throat.
• Back pain.
• Night sweats.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

If overdose is suspected:

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.

How do I store and/or throw out pralatrexate?

• If you need to store pralatrexate at home, talk with your doctor, nurse, or pharmacist about how to store it.

Label

PACKAGE CARTON – FOLOTYN 20 mg/1 mL Vial

• NDC 72893-003-01
  FOLOTYN®
• (pralatrexate injection)
• 20 mg/mL
• For intravenous use
• Rx only
• 1 mL

 

PACKAGE CARTON – FOLOTYN 40 mg/2 mL Vial

• NDC 72893-005-01
• FOLOTYN®
• (pralatrexate injection)
• 40 mg/2 mL
• (20 mg/mL)
• For intravenous use
• Rx only
• 2 mL

SRC: NLM .