Drug intelligence / Profile preview

cisplatin + gemcitabine + rofecoxib

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This drug is a combination chemotherapy regimen consisting of three agents: - **Cisplatin** is a platinum-based chemotherapy drug that causes DNA crosslinking and damage, leading to apoptosis in rapidly dividing cancer cells. It is used widely in various cancers including bladder, lung, ovarian, cervical, and biliary tract cancers. - **Gemcitabine** is a nucleoside analog that inhibits DNA synthesis by incorporation into DNA strands and inhibition of ribonucleotide reductase. It acts as an antimetabolite chemotherapy agent effective against multiple solid tumors such as non-small cell lung cancer (NSCLC), bladder cancer, pancreatic cancer, and gallbladder cancer. - **Rofecoxib** was a selective cyclooxygenase-2 (COX-2) inhibitor nonsteroidal anti-inflammatory drug (NSAID) formerly used for osteoarthritis and pain relief but withdrawn from the market due to cardiovascular risk concerns. Its inclusion in this combination likely aimed at exploiting COX-2 inhibition's potential role in modulating tumor microenvironment or inflammation associated with cancer progression. The combination leverages the cytotoxic effects of cisplatin and gemcitabine on tumor cells along with the anti-inflammatory action of rofecoxib. Cisplatin plus gemcitabine has demonstrated efficacy in advanced cancers such as NSCLC, gallbladder cancer, bladder cancer among others. Rofecoxib’s role would be adjunctive but it was withdrawn from clinical use due to safety issues.

Other names
GC plus rofecoxibgemcitabine-cisplatin combined with rofecoxib
02

Targets

DNAPTGS2 (Prostaglandin-Endoperoxide Synthase 2)DNA polymerase familyRNR (Ribonucleotide reductase)

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