Drug intelligence / Profile preview

AS703569 + gemcitabine

Development stage
Phase 1
Lead developer
Merck KGaA
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

AS703569 + gemcitabine is an investigational combination therapy for cancer. AS703569 (also known as R763) is a highly potent, orally available small molecule inhibitor of Aurora kinase A and Aurora kinase B, as well as several other kinases. Aurora kinases are critical regulators of mitosis and are implicated in tumorigenesis; their inhibition disrupts cell division and induces apoptosis in cancer cells[6][8]. Gemcitabine is a nucleoside analog antimetabolite chemotherapeutic agent that inhibits DNA synthesis by incorporating into DNA during replication, leading to cell cycle arrest and apoptosis[4]. Gemcitabine is approved for use in various cancers including pancreatic, ovarian, breast, and non-small cell lung cancer[1][3][4]. The combination has been studied in early-phase clinical trials for advanced malignancies such as pancreatic, ovarian, breast, non-small cell lung cancer (NSCLC), and colorectal cancers[8].

Brand names
Gemzar
02

Targets

AURKA (Aurora kinase A)AURKB (Aurora kinase B)DNA polymerase familyRNR (Ribonucleotide reductase)

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