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Updated: Jul 29, 2026

Development and Maintenance of a Preclinical Patient Derived Tumor Xenograft Model for the Investigation of Novel Anti-Cancer Therapies
Published on: September 30, 2016
Orally bioavailable farnesyltransferase inhibitors as anticancer agents in transgenic and xenograft models
M Liu1, W R Bishop, L L Nielsen
1Schering-Plough Research Institute, Kenilworth, New Jersey 07033-1300, USA.
Abstract:
The in vivo evaluation process described here was instrumental in the identification of SCH 66336 as a clinical candidate. Our lead FTI, SCH 66336, and several other FTIs are being evaluated in early-phase clinical trials to establish proof-of-principle for farnesyl transferase inhibition in human patients. The preclinical studies described here suggest that FTIs may have utility against a wide array of human cancers as a single agent and may, at least in some cases, lead to tumor regression. In addition, the results to date in combination with cytotoxic chemotherapeutic agents in animal models indicate that these combinations may enhance the clinical efficacy of FPT inhibitors. Further preclinical studies should help to guide the clinical development of this class of novel antitumor agents.
Insights
Farnesyl transferase inhibitors (FTIs) like SCH 66336 show promise in preclinical cancer models. Further studies are needed to guide clinical development of these novel antitumor agents.
Area of Science:
- Oncology
- Pharmacology
Background:
- Farnesyl transferase inhibitors (FTIs) are a novel class of anticancer agents.
- SCH 66336 is a lead FTI identified through in vivo evaluation.
Purpose of the Study:
- To evaluate the preclinical efficacy of FTIs, including SCH 66336.
- To explore the potential of FTIs as single agents and in combination therapy for various human cancers.
Main Methods:
- In vivo evaluation of SCH 66336 and other FTIs in preclinical cancer models.
- Assessment of FTIs as single agents and in combination with cytotoxic chemotherapy.
Main Results:
- Preclinical studies suggest FTIs may be effective against a broad spectrum of human cancers.
- Tumor regression was observed in some cases with FTI monotherapy.
- Combination therapy with cytotoxic agents showed enhanced efficacy in animal models.
Conclusions:
- FTIs, including SCH 66336, demonstrate potential as antitumor agents for diverse cancers.
- Combination strategies may improve the clinical efficacy of FPT inhibitors.
- Further preclinical research is crucial for guiding the clinical development of FTIs.
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