Drug intelligence / Profile preview

C75

Development stage
Discontinued
Lead developer
Johns Hopkins University
Modality
Small Molecules
Administration
Oral, Intraperitoneal
01

Overview

C75 is a synthetic small molecule inhibitor of fatty acid synthase (FASN), a multi-enzyme complex responsible for the de novo synthesis of long-chain fatty acids. Originally developed at Johns Hopkins University, C75 was primarily investigated for its potent anti-obesity and anti-tumor properties. Its mechanism involves the irreversible inhibition of the ketoacyl synthase domain of FASN, which leads to a significant accumulation of the substrate malonyl-CoA. In the central nervous system, particularly the hypothalamus, this increase in malonyl-CoA levels signals a state of energy surplus, thereby suppressing appetite and increasing energy expenditure. In oncology, C75 induces apoptosis in cancer cells that rely on high rates of fatty acid synthesis for membrane production and signaling, such as those found in breast, prostate, and ovarian cancers. Despite its efficacy in animal models, C75 has not progressed to clinical trials due to significant side effects, including profound weight loss and potential systemic toxicity, and it remains widely used as a pharmacological tool in metabolic and cancer research.

Other names
alpha-methylene-2-octyl-5-oxotetrahydrofuran-3-carboxylic acidalpha-methylene2-octyl-5-oxotetrahydrofuran-3-carboxylic acidalpha-methylene 2-octyl-5-oxotetrahydrofuran-3-carboxylic acidtrans-tetrahydro-4-methylene-2-octyl-5-oxo-3-furancarboxylic acidtrans-tetrahydro4-methylene-2-octyl-5-oxo-3-furancarboxylic acidtrans-tetrahydro 4-methylene-2-octyl-5-oxo-3-furancarboxylic acid
02

Targets

FASN (Fatty acid synthase)SLC7A1 (Cationic amino acid transporter 1)

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