Drug intelligence / Profile preview

pemetrexed (Eli Lilly and Company)

Development stage
Approved
Lead developer
Eli Lilly
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Pemetrexed is a small molecule chemotherapy drug classified as an antifolate antineoplastic agent. It is primarily used to treat malignant pleural mesothelioma and non-squamous non-small cell lung cancer (NSCLC), either alone or in combination with other agents such as cisplatin or pembrolizumab[1][2][3]. Pemetrexed works by inhibiting several folate-dependent enzymes essential for DNA and purine synthesis—specifically thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT)[3][6][8]. This inhibition disrupts DNA replication and repair in rapidly dividing cancer cells. The drug is administered intravenously, typically every 21 days, and patients often receive supplemental folic acid, vitamin B12, and corticosteroids to reduce side effects[2][5]. Pemetrexed was developed by Eli Lilly and Company.

Brand names
AlimtaPemfexyPemrydi RTUAxtle
Other names
pemetrexed disodium
02

Targets

GART (GAR transformylase)DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)

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