Drug intelligence / Profile preview

ARQ 501 + gemcitabine

Development stage
Phase 2
Lead developer
Merck
Modality
Small Molecules
Administration
Intravenous
01

Overview

ARQ 501 (β-Lapachone) is a novel small molecule anticancer agent that induces apoptosis in cancer cells by modulating the expression of E2F transcription factor 1, thereby activating the G1/S-phase checkpoint. It also acts as a topoisomerase I inhibitor and inhibits cell cycle progression. Gemcitabine is a nucleoside analog antimetabolite used in chemotherapy, which works by inhibiting DNA synthesis and slowing or stopping the growth of cancer cells. The combination of ARQ 501 and gemcitabine has been investigated for synergistic effects in treating cancers such as pancreatic cancer, particularly in patients with unresectable disease[2][3][6]. ARQ 501 was developed by ArQule (now part of Merck), while gemcitabine is marketed under various brand names for multiple solid tumors.

Other names
beta-LapachoneNSC-26326NSC26326NSC 26326
02

Targets

SLC28A1 (Sodium/nucleoside cotransporter 1)DNA polymerase familyE2F1 (E2F Transcription Factor 1)ENT1 (Solute carrier family 29 member 1)TOP1 (DNA Topoisomerase I)

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