TAS3681 / Otsuka - LARVOL DELTA

TO-TAS3681-101: Study of TAS3681 in Metastatic Castration Resistant Prostate Cancer (clinicaltrials.gov) - P1 | N=130 | Completed | Sponsor: Taiho Oncology, Inc. | Active, not recruiting ➔ Completed

Metastases • Trial completion • Genito-urinary Cancer • Metastatic Castration-Resistant Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor

TAS3681, an androgen receptor antagonist, prevents drug resistance driven by aberrant androgen receptor signaling in prostate cancer. (PubMed, Mol Oncol) - "Second-generation androgen receptor (AR) signaling inhibitors (ARSIs), such as abiraterone and enzalutamide, prolong the life of patients with castration-resistant prostate cancer (CRPC)...Importantly, TAS3681 blocked the transcriptional activity of various mutant ARs, including mutations F877L/T878A and H875Y/T878A, which confer resistance to enzalutamide, and V716M and H875Y mutations, which confer resistance to darolutamide. Our results demonstrate that TAS3681 suppresses the reactivation of AR signaling, which causes resistance to ARSIs, via a newly identified mechanism of action. Therefore, TAS3681 could be a new therapeutic option for CRPC treatment."

Journal • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

TO-TAS3681-101: Study of TAS3681 in Metastatic Castration Resistant Prostate Cancer (clinicaltrials.gov) - P1 | N=130 | Active, not recruiting | Sponsor: Taiho Oncology, Inc. | N=200 ➔ 130 | Trial completion date: Oct 2023 ➔ Mar 2024

Enrollment change • Metastases • Trial completion date • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

TO-TAS3681-101: Study of TAS3681 in Metastatic Castration Resistant Prostate Cancer (clinicaltrials.gov) - P1 | N=200 | Active, not recruiting | Sponsor: Taiho Oncology, Inc. | Trial completion date: Oct 2022 ➔ Oct 2023 | Trial primary completion date: Sep 2022 ➔ Sep 2023

Metastases • Trial completion date • Trial primary completion date • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

TO-TAS3681-101: Study of TAS3681 in Metastatic Castration Resistant Prostate Cancer (clinicaltrials.gov) - P1 | N=200 | Active, not recruiting | Sponsor: Taiho Oncology, Inc. | Recruiting ➔ Active, not recruiting

Enrollment closed • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Study of TAS3681 in Metastatic Castration Resistant Prostate Cancer (clinicaltrials.gov) - P1; N=200; Recruiting; Sponsor: Taiho Oncology, Inc.; Trial completion date: Sep 2021 ➔ Oct 2022; Trial primary completion date: Sep 2021 ➔ Sep 2022

Clinical • Trial completion date • Trial primary completion date • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Study of TAS3681 in Metastatic Castration Resistant Prostate Cancer (clinicaltrials.gov) - P1; N=200; Recruiting; Sponsor: Taiho Oncology, Inc.; N=130 ➔ 200; Trial completion date: Jun 2019 ➔ Sep 2021; Trial primary completion date: Jun 2019 ➔ Sep 2021

Clinical • Enrollment change • Trial completion date • Trial primary completion date • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Study of TAS3681 in Metastatic Castration Resistant Prostate Cancer (clinicaltrials.gov) - P1; N=130; Recruiting; Sponsor: Taiho Oncology, Inc.; Trial completion date: Jun 2018 ➔ Jun 2019; Trial primary completion date: Jun 2017 ➔ Jun 2019

Clinical • Trial completion date • Trial primary completion date • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Study of TAS3681 in Metastatic Castration Resistant Prostate Cancer (clinicaltrials.gov) - P1; N=130; Recruiting; Sponsor: Taiho Oncology, Inc.; Not yet recruiting ➔ Recruiting

Clinical • Enrollment open • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Study of TAS3681 in Metastatic Castration Resistant Prostate Cancer (clinicaltrials.gov) - P1; N=130; Not yet recruiting; Sponsor: Taiho Oncology, Inc.

Clinical • New P1 trial • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

[VIRTUAL] First-in-human study of TAS3681, an oral androgen receptor (AR) antagonist with AR and AR splice variant (AR-SV) downregulation activity, in patients (pts) with metastatic castration-resistant prostate cancer (mCRPC) refractory to abiraterone (ABI) and/or enzalutamide (ENZ) and chemotherapy (CT). (ASCO 2021) - P1 | "The recommended phase 2 dose is 300 mg BID . TAS3681 has a manageable safety profile and has antitumor activity against heavily pretreated, multi-drug resistant mCRPC . The study expansion phase is enrolling pts who have progressed on ABI or ENZ +/- taxane CT."

Clinical • P1 data • Fatigue • Genito-urinary Cancer • Hepatology • Hypertension • Oncology • Prostate Cancer • Solid Tumor • AR

"@TaihoOncology select 300 mg BID dose of oral AR antagonist TAS3681 as best dosage candidate for further development #ASCO2021" (@Cortellis)

Oncology

AR-V7 in Metastatic Prostate Cancer: A Strategy beyond Redemption. (PubMed, Int J Mol Sci) - "AR-V7 is an important oncogenic driver and plays a role as an early diagnostic and prognostic marker, as well as a therapeutic target for antagonists such as niclosamide and TAS3681. Anti-AR-V7 drugs have shown promise in recent clinical investigations on this subset of patients. This mini-review focuses on the relevance of AR-V7 in the clinical manifestations of castration-resistant prostate cancer (CRPC) and summarizes redemptive therapeutic strategies."

Journal • Review • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • AR