Drug intelligence / Profile preview

pemetrexed + mitomycin + tamoxifen + estradiol

Development stage
Preclinical
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a **combination drug** containing four active pharmaceutical ingredients: **pemetrexed**, **mitomycin**, **tamoxifen**, and **estradiol**. - **Pemetrexed** is a folate analog antimetabolite that inhibits thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase, disrupting folate-dependent processes essential for DNA and RNA synthesis, leading to cell death in rapidly dividing tumor cells[9]. - **Mitomycin** (typically mitomycin C) is an alkylating agent that cross-links DNA, inhibiting DNA synthesis and function. - **Tamoxifen** is a selective estrogen receptor modulator (SERM) that acts as an estrogen receptor antagonist in breast tissue, thereby inhibiting estrogen-dependent proliferation of breast cancer cells. In other tissues, it can have partial agonist effects[3][7][10]. - **Estradiol** is the principal estrogen hormone and acts as an agonist of the estrogen receptor. There are no approved combination products or notable clinical studies specifically combining all four agents (pemetrexed + mitomycin + tamoxifen + estradiol) as a marketed preparation. Some combinations of mitomycin and tamoxifen have been reported in breast cancer treatment, but not with pemetrexed or estradiol together[1][5].

02

Targets

TS (Thymidylate synthase)GART (GAR transformylase)DHFR (Dihydrofolate reductase)DNAESR2 (ERβ)ESR1 (ERα)ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)

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