Drug intelligence / Profile preview

gemcitabine + cisplatin

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Gemcitabine + cisplatin is a chemotherapy combination regimen used to treat several types of cancer, including non-small cell lung cancer, biliary tract cancer, bladder cancer, cervical cancer, malignant mesothelioma, ovarian cancer, and pancreatic cancer. Gemcitabine is an antimetabolite that mimics nucleosides and disrupts DNA synthesis by being incorporated into DNA strands during replication, leading to masked chain termination and inhibition of further DNA synthesis. It also inhibits ribonucleotide reductase via its diphosphate form. Cisplatin is an alkylating agent that forms crosslinks in DNA strands and prevents cell division by causing irreparable damage to the genetic material. The combination exploits different mechanisms to destroy rapidly dividing cells more effectively than either drug alone.

Brand names
Gemzar
Other names
GEMCITABINE-CISPLATINCISplatin-Gemcitabine
02

Targets

POLA1 (DNA polymerase alpha)RNR (Ribonucleotide reductase)

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