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FASN as a target


FASN is responsible for synthesizing palmitate. In tumor cells, and some virus infected cells, palmitate derived from FASN is:

  • Used directly as an energy source
  • Converted to more specific fatty acids and lipids that either directly transmit signals or modify proteins (e.g., Wnt and NRAS) that transmit cellular growth and survival signals
  • Converted into more complex fatty acids and lipids that are used to build cellular membranes

FASN as a therapeutic target in oncology is supported by a number of different observations:

  • FASN is increased in the bloodstream and tumors of patients with a variety of cancers
  • Patients with high levels of FASN have higher mortality rate than those with lower levels of FASN
  • Increased expression of FASN in preclinical models can lead to tumor formation
  • Blocking FASN can inhibit tumor growth in many tumor types, including breast, lung and colorectal tumors
  • FASN inhibition is well tolerated at pharmacologically active levels

FASN, a well-credentialed target in oncology, has long been a target of interest in the pharmaceutical industry. Our internal medicinal chemistry team has created FASN inhibitors that are orally available, selective, potent and reversible. Based on these characteristics, we have advanced our lead product candidate TVB-2640 as the first-in-class  FASN inhibitor into a Phase 1 clinical trial. We have established the preliminary safety profile, defined the maximally tolerated dose (MTD) and demonstrated target engagement in patients. We are now expanding the trial to enroll multiple cohorts of patients with specific tumor types.