PEMETREXED

Other

Brand names: Pemfexy

Intravenous

Mechanism of Action

12.1 Mechanism of Action Pemetrexed is a folate analog metabolic inhibitor that disrupts folate-dependent metabolic processes essential for cell replication. In vitro studies show that pemetrexed inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), which are folate-dependent enzymes involved in the de novo biosynthesis of thymidine and purine nucleotides. Pemetrexed is taken into cells by membrane carriers, such as 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.

Indications

1 INDICATIONS AND USAGE PEMFEXY™ is a folate analog metabolic inhibitor indicated for: in combination with pembrolizumab and platinum chemotherapy

for the initial treatment of patients with metastatic non-squamous NSCLC

with no EGFR or ALK genomic tumor aberrations. ( 1.1 ) in combination with cisplatin for the initial treatment of patients with locally advanced or metastatic non-squamous

for the initial treatment of patients with metastatic non-squamous non-small cell lung cancer (NSCLC)

with no EGFR or ALK genomic tumor aberrations. in combination with cisplatin for the initial treatment of patients with locally advanced or metastatic

FDA Warnings

5 WARNINGS AND PRECAUTIONS Myelosuppression : Can cause severe bone marrow suppression resulting in cytopenia and an increased risk of infection
1 ) Renal Failure : Can cause severe, and sometimes fatal, renal failure
Advise patients of the potential risk to a fetus and to use effective contraception
1 Myelosuppression and Increased Risk of Myelosuppression without Vitamin Supplementation Pemetrexed can cause severe myelosuppression resulting in a requirement for transfusions and which may lead to neutropenic infection

Known Side Effects

6 documented side effects by frequency

Nausea

1-10%

Diarrhea

1-10%

Fatigue

1-10%

Vomiting

1-10%

Shortness of Breath

1-10%

Fever

0.1-1%

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Formulations

Dosage Forms

Tablet

Route

Intravenous