Drug intelligence / Profile preview

RP-6306 + FOLFIRI

Development stage
Unknown
Lead developer
Repare Therapeutics
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

**RP-6306 + FOLFIRI** is an investigational combination therapy consisting of RP-6306, a selective small-molecule inhibitor of PKMYT1, and the established chemotherapeutic regimen FOLFIRI, which includes folinic acid (leucovorin), fluorouracil (5-fluorouracil, 5-FU), and irinotecan. RP-6306 targets PKMYT1, a kinase involved in cell cycle regulation, with the aim of selectively inhibiting the proliferation of cancer cells, particularly those with specific genetic alterations. FOLFIRI is a cytotoxic regimen that interferes with DNA synthesis and cell division, primarily through the actions of 5-FU and irinotecan, supported by leucovorin to enhance 5-FU efficacy. The combination is being investigated for use in patients with advanced solid tumors, notably those resistant to standard therapies, to evaluate safety, dose, and preliminary efficacy[1][3][5].

02

Targets

TOP1 (DNA Topoisomerase I)PKMYT1 (Protein kinase membrane associated tyrosine/threonine 1)TS (Thymidylate synthase)

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