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Updated: Mar 14, 2026

Author Spotlight: Establishing MASLD Cell Models for Investigating Disease Mechanisms and the Lipid-Lowering Effects of Koumiss
Published on: July 19, 2024
Recent advances in targeting the fatty acid biosynthetic pathway using fatty acid synthase inhibitors
Thelma S Angeles1, Robert L Hudkins1
1a Discovery and Product Development , Teva Branded Pharmaceutical Products R&D, Inc ., West Chester , PA , USA.
Introduction:
Elevated lipogenesis has been associated with a variety of diseases including obesity, cancer and nonalcoholic fatty liver disease (NAFLD). Fatty acid synthase (FASN) plays a pivotal role in de novo lipogenesis, making this multi-catalytic protein an attractive target for therapeutic intervention. Recently, the first FASN inhibitor successfully advanced through the drug development process and entered clinical evaluation in oncology. Areas covered: This review discusses the biological roles of FASN in three prominent disease areas: cancer, obesity-related disorders and NAFLD. Recent advances in drug discovery strategies and design of newer FASN inhibitors are also highlighted. Expert opinion: Despite the abundance of evidence linking the lipogenic pathway to cancer, progression of FASN-targeted molecules has been rather slow and challenging and no compounds have moved past the preclinical phase. The landscape has recently changed with the recent advancement of the first FASN inhibitor into clinical evaluation for solid tumors. Needless to say, the successful translation into the clinical setting will open opportunities for expanding the therapeutic utility of FASN inhibitors not just in oncology but in other diseases associated with elevated lipogenesis such as obesity, type 2 diabetes, and NAFLD.
Insights
Fatty acid synthase (FASN) is crucial in lipogenesis, a process linked to diseases like cancer and NAFLD. New FASN inhibitors show promise for treating these conditions, with one now in clinical trials for solid tumors.
Area of Science:
- Biochemistry
- Pharmacology
- Oncology
Background:
- Elevated lipogenesis is implicated in diseases such as obesity, cancer, and nonalcoholic fatty liver disease (NAFLD).
- Fatty acid synthase (FASN), a key enzyme in de novo lipogenesis, is a significant therapeutic target.
- The development of FASN inhibitors has progressed, with the first entering clinical trials for oncology.
Purpose of the Study:
- To review the biological roles of FASN in cancer, obesity-related disorders, and NAFLD.
- To highlight recent advancements in drug discovery and the design of novel FASN inhibitors.
- To discuss the therapeutic potential of FASN inhibitors beyond oncology.
Main Methods:
- Literature review of FASN's role in disease pathogenesis.
- Analysis of recent drug discovery strategies for FASN inhibitors.
- Evaluation of clinical trial data for FASN-targeted therapies.
Main Results:
- FASN plays a critical role in the progression of cancer, obesity, and NAFLD.
- Despite challenges, the first FASN inhibitor has advanced to clinical evaluation in oncology.
- Newer FASN inhibitors are being developed with improved strategies.
Conclusions:
- FASN inhibition represents a promising therapeutic strategy for cancer, obesity, and NAFLD.
- The clinical advancement of FASN inhibitors opens new avenues for treating lipogenesis-related diseases.
- Further research into FASN inhibitors could expand their clinical utility across multiple disease areas.
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