Drug intelligence / Profile preview

CRLX101 + capecitabine

Development stage
Preclinical
Lead developer
Daré Bioscience
Modality
Small Molecules, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous, Oral
01

Overview

CRLX101 + capecitabine is a combination therapy consisting of CRLX101, a nanopharmaceutical drug conjugate, and capecitabine, an oral chemotherapeutic agent. CRLX101 is a nanoparticle conjugate composed of a cyclodextrin-based polymer (CDP) delivery molecule and camptothecin (CPT), an anti-cancer compound. This nanomedicine design allows preferential accumulation in tumor tissues while reducing systemic toxicity. The nanoparticle structure enables CRLX101 to enter cancer cells through endosomal pathways, creating an intracellular CPT depot with sustained release. CRLX101 works by inhibiting topoisomerase I and hypoxia-inducible factor 1-alpha (HIF-1α), leading to downregulation of carbonic anhydrase IX (CA IX). Capecitabine is an oral fluoropyrimidine that is converted to 5-fluorouracil in tumor tissues.

02

Targets

TOP1 (DNA Topoisomerase I)TS (Thymidylate synthase)HIF1A (Hypoxia-inducible factor 1-alpha)

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