TAVT-45 is an enhanced formulation of abiraterone acetate and is in development as a treatment for prostate cancer.

TAVT-45 was developed using our HT Matrix Screening Platform as an improved formulation of the commercially available ZYTIGA® (abiraterone acetate) tablets. All currently available formulations of abiraterone acetate necessitate ingestion of multiple large tablets. TAVT-45 offers an alternative to patients who have difficulty swallowing.

Abiraterone acetate, a prodrug of abiraterone, is indicated for the treatment of metastatic castration-resistant prostate cancer and high-risk metastatic castration-sensitive prostate cancer, in combination with prednisone. Abiraterone inhibits testosterone production, which can suppress tumor growth.

In addition to the multiple large tablets required daily, other limitations of Zytiga® include the requirement to be taken on an empty stomach and the high variability in systemic exposure. This high variability has been shown to result in patients with low abiraterone plasma concentrations and exposure, which can lead to suboptimal clinical outcomes.1, 2

In single dose clinical Phase 1 safety and pharmacokinetic studies with TAVT-45, variability in abiraterone exposure was reduced compared to Zytiga®, and bioavailability was enhanced in subjects in a fasted state. TAVT-45 was also shown to be well tolerated. Overall, it is expected that TAVT-45 may eliminate the requirement of taking the drug on an empty stomach, allow for a reduction in the total daily dose of abiraterone compared to Zytiga®, and may result in a lower proportion of patients having sub-optimal abiraterone trough concentrations.

1 Carton E, Noe G, Huillard O, et al. Relation between plasma trough concentration of abiraterone and prostate-specific antigen response in metastatic castration-resistant prostate cancer patients. Eur J Cancer. 2017;72:54-61.
2 van Nuland M, Groenland SL, Bergman AM, et al. Exposure-response analyses of abiraterone and its metabolites in real-world patients with metastatic castration-resistant prostate cancer. Prostate Cancer Prostatic Dis. 2020;23(2):244-251.