Alimta

Alimta - General Information

Alimta (brand name Alimta®) is a chemotherapy drug manufactured and marketed by Eli Lilly and Company. Its indications are the treatment of pleural mesothelioma as well as non-small cell lung cancer.

Pharmacology of Alimta

Preclinical studies have shown that pemetrexed inhibits the in vitro growth of mesothelioma cell lines (MSTO-211H, NCI-H2052). Studies with the MSTO-211H mesothelioma cell line showed synergistic effects when pemetrexed was combined concurrently with cisplatin.

Alimta for patients

INFORMATION FOR PATIENTS AND CAREGIVERS

ALIMTA (uh-LIM-tuh)

(pemetrexed for injection)

Read the Patient Information that comes with ALIMTA before you start treatment and each time you get treated with ALIMTA. There may be new information. This leaflet does not take the place of talking to your doctor about your medical condition or treatment. Talk to your doctor if you have any questions about ALIMTA.

What is ALIMTA?

ALIMTA is a treatment for:

• Malignant pleural mesothelioma. This cancer affects the inside lining of the chest cavity. ALIMTA is given with cisplatin, another anti-cancer medicine (chemotherapy).

• Non-small cell lung cancer. This cancer is a disease in which malignant (cancer) cells form in the tissues of the lung.

To lower your chances of side effects of ALIMTA, you must also take folic acid and vitamin B₁₂ prior to and during your treatment with ALIMTA. Your doctor will prescribe a medicine called a "corticosteroid" to take for 3 days during your treatment with ALIMTA. Corticosteroid medicines lower your chances of getting skin reactions with ALIMTA.

ALIMTA has not been studied in children.

What should I tell my doctor before taking ALIMTA?

Tell your doctor about all of your medical conditions, including if you:

• are pregnant or planning to become pregnant. ALIMTA may harm your unborn baby.

• are breastfeeding. It is not known if ALIMTA passes into breast milk. You should stop breastfeeding once you start treatment with ALIMTA.

• are taking other medicines, including prescription and nonprescription medicines, vitamins, and herbal supplements. ALIMTA and other medicines may affect each other causing serious side effects. Especially, tell your doctor if you are taking medicines called "nonsteroidal anti-inflammatory drugs" (NSAIDs) for pain or swelling. There are many NSAID medicines. If you are not sure, ask your doctor or pharmacist if any of your medicines are NSAIDs.

How is ALIMTA given?

• ALIMTA is slowly infused (injected) into a vein. The injection or infusion will last about 10 minutes. You will usually receive ALIMTA once every 21 days (3 weeks).

• If you are being treated for malignant pleural mesothelioma, ALIMTA is given in combination with cisplatin (another anti-cancer drug). Cisplatin is infused in your vein for about 2 hours starting about 30 minutes after your treatment with ALIMTA.

• Your doctor will prescribe a medicine called a "corticosteroid" to take for 3 days during your treatment with ALIMTA. Corticosteroid medicines lower your chances for getting skin reactions with ALIMTA.

• It is very important to take folic acid and vitamin B₁₂ during your treatment with ALIMTA to lower your chances of harmful side effects. You must start taking 350-1000 micrograms of folic acid every day for at least 5 days out of the 7 days before your first dose of ALIMTA. You must keep taking folic acid every day during the time you are getting treatment with ALIMTA, and for 21 days after your last treatment. You can get folic acid vitamins over-the-counter. Folic acid is also found in many multivitamin pills. Ask your doctor or pharmacist for help if you are not sure how to choose a folic acid product. Your doctor will give you vitamin B₁₂ injections while you are getting treatment with ALIMTA. You will get your first vitamin B₁₂ injection during the week before your first dose of ALIMTA, and then about every 9 weeks during treatment.

• You will have regular blood tests before and during your treatment with ALIMTA. Your doctor may adjust your dose of ALIMTA or delay treatment based on the results of your blood tests and on your general condition.

What should I avoid while taking ALIMTA?

• Women who can become pregnant should not become pregnant during treatment with ALIMTA. ALIMTA may harm the unborn baby.

• Ask your doctor before taking medicines called NSAIDs. There are many NSAID medicines. If you are not sure, ask your doctor or pharmacist if any of your medicines are NSAIDs.

What are the possible side effects of ALIMTA?

Most patients taking ALIMTA will have side effects. Sometimes it is not always possible to tell whether ALIMTA, another medicine, or the cancer itself is causing these side effects. Call your doctor right away if you have a fever, chills, diarrhea, or mouth sores. These symptoms could mean you have an infection.

The most common side effects of ALIMTA when given alone or in combination with cisplatin are:

• Stomach upset, including nausea, vomiting, and diarrhea. You can obtain medicines to help control some of these symptoms. Call your doctor if you get any of these symptoms.

• Low blood cell counts:

• Low red blood cells. Low red blood cells may make you feel tired, get tired easily, appear pale, and become short of breath.

• Low white blood cells. Low white blood cells may give you a greater chance for infection. If you have a fever (temperature above 100.4°F) or other signs of infection, call your doctor right away.

• Low platelets. Low platelets give you a greater chance for bleeding. Your doctor will do blood tests to check your blood counts before and during treatment with ALIMTA.

• Tiredness. You may feel tired or weak for a few days after your ALIMTA treatments. If you have severe weakness or tiredness, call your doctor.

• Mouth, throat, or lip sores (stomatitis, pharyngitis). You may get redness or sores in your mouth, throat, or on your lips. These symptoms may happen a few days after ALIMTA treatment. Talk with your doctor about proper mouth and throat care.

• Loss of appetite. You may lose your appetite and lose weight during your treatment. Talk to your doctor if this is a problem for you.

• Rash. You may get a rash or itching during treatment. These usually appear between treatments with ALIMTA and usually go away before the next treatment. Call your doctor if you get a severe rash or itching. Talk with your doctor, nurse or pharmacist about any side effect that bothers you or that doesn’t go away.

These are not all the side effects of ALIMTA. For more information, ask your doctor, nurse or pharmacist.

General information about ALIMTA

Medicines are sometimes prescribed for conditions other than those listed in patient information leaflets. ALIMTA was prescribed for your medical condition.

This leaflet summarizes the most important information about ALIMTA. If you would like more information, talk with your doctor. You can ask your doctor or pharmacist for information about ALIMTA that is written for health professionals. You can also call 1-800-LILLY-RX (1-800-545-5979) or visit www.ALIMTA.com.

Alimta Interactions

ALIMTA is primarily eliminated unchanged renally as a result of glomerular filtration and tubular secretion. Concomitant administration of nephrotoxic drugs could result in delayed clearance of ALIMTA. Concomitant administration of substances that are also tubularly secreted (e.g., probenecid) could potentially result in delayed clearance of ALIMTA.

Although ibuprofen (400 mg qid) can be administered with ALIMTA in patients with normal renal function (creatinine clearance ³80 mL/min), caution should be used when administering ibuprofen concurrently with ALIMTA to patients with mild to moderate renal insufficiency (creatinine clearance from 45 to 79 mL/min). Patients with mild to moderate renal insufficiency should avoid taking NSAIDs with short elimination half-lives for a period of 2 days before, the day of, and 2 days following administration of ALIMTA.

In the absence of data regarding potential interaction between ALIMTA and NSAIDs with longer half-lives, all patients taking these NSAIDs should interrupt dosing for at least 5 days before, the day of, and 2 days following ALIMTA administration. If concomitant administration of an NSAID is necessary, patients should be monitored closely for toxicity, especially myelosuppression, renal, and gastrointestinal toxicity.

Drug/Laboratory Test Interactions

None known.

Alimta Contraindications

ALIMTA is contraindicated in patients who have a history of severe hypersensitivity reaction to pemetrexed or to any other ingredient used in the formulation.

Additional information about Alimta

Alimta Indication: For the treatment of malignant pleural mesothelioma and locally advanced or metastatic non-small cell lung cancer (NSCLC) after prior chemotherapy
Mechanism Of Action: Alimta is an antifolate containing the pyrrolopyrimidine-based nucleus that exerts its antineoplastic activity by disrupting folate-dependent metabolic processes essential for cell replication. In vitro studies have shown that pemetrexed inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), all folate-dependent enzymes involved in the de novo biosynthesis of thymidine and purine nucleotides. Alimta is transported into cells by both the reduced folate carrier and membrane folate binding protein transport systems. Once in the cell, pemetrexed is converted to polyglutamate forms by the enzyme folylpolyglutamate synthetase. The polyglutamate forms are retained in cells and are inhibitors of TS and GARFT. Polyglutamation is a time- and concentration-dependent process that occurs in tumor cells and, to a lesser extent, in normal tissues. Polyglutamated metabolites have an increased intracellular half-life resulting in prolonged drug action in malignant cells.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Pemetrexed
Synonyms: LY231514; Pemetrexed Disodium
Drug Category: Antineoplastic Agents; Antimetabolites; Enzyme Inhibitors; Folic Acid Antagonists
Drug Type: Small Molecule; Approved; Investigational

Other Brand Names containing Pemetrexed: Alimta;
Absorption: Not Available
Toxicity (Overdose): Not Available
Protein Binding: 81%
Biotransformation: Metabolized by Cytochrome P450 Enzymes
Half Life: 3.5 hours
Dosage Forms of Alimta: Powder, for solution Intravenous
Chemical IUPAC Name: (2R)-2-[[4-[2-(2-amino-4-oxo-1,7-dihydropyrrolo[4,5-e]pyrimidin-5-yl)ethyl]benzoyl]amino]pentanedioic acid
Chemical Formula: C20H21N5O6
Pemetrexed on Wikipedia: https://en.wikipedia.org/wiki/Pemetrexed
Organisms Affected: Humans and other mammals