• Androgen Receptor (AR) inhibition is an important therapeutic approach for the treatment of Castration-Resistant Prostate Cancer (CRPC), but AR-escape mechanisms related to the expression of AR splice variants (AR-SV), such as AR-V7, represent a significant unmet need and are a key area of focus for novel therapies in development
  • ONCT-534 may become a promising next-generation treatment option for CRPC and for the clinically-important emerging class of AR-SV-expressing prostate cancers

SAN DIEGO, CA, USA I October 05, 2021 I Oncternal Therapeutics, Inc. (Nasdaq: ONCT), a clinical-stage biopharmaceutical company focused on the development of novel oncology therapies, today announced pre-clinical data from ONCT-534, an androgen receptor N-terminal-domain-binding small molecule degrader, was accepted for virtual poster presentation at the AACR-NCI-EORTC Virtual International Conference on Molecular Targets and Cancer Therapeutics on October 7-10, 2021. Oncternal has conducted a series of preclinical studies in collaboration with the Center for Cancer Research at the University of Tennessee Health Science Center.

The ONCT-534 data will be presented as a late-breaking abstract selected for virtual poster presentations and will be available for on-demand viewing in the AACR-NCI-EORTC platform on October 7, 2021, at 9 a.m. ET.

  • Abstract Title: Androgen Receptor (AR) N-Terminus-Domain-Binding Small Molecule Degraders for the Treatment of AR Splice Variant-Positive Castration-Resistant Prostate Cancer
  • Abstract Number: LBA016

“Despite relatively recent advances in treating CRPC, 5-year overall survival remains low, and patients are in need of more effective treatment options” said James Breitmeyer, M.D., Ph.D., Oncternal’s President and CEO. “In preclinical research, ONCT-534 has demonstrated anti-tumor activity in a series of studies and might have the potential to address significant unmet needs related to important tumor resistance mechanisms, including those involving expression of the AR splice variant AR-V7.”

About ONCT-534

ONCT-534 (formerly GTx-534) is an investigational, potentially first-in-class androgen receptor (AR) N-terminal-domain-binding small molecule degrader, currently in preclinical development, that was originally discovered by the Center for Cancer Research at the University of Tennessee Health Science Center. Oncternal acquired rights to ONCT-534, which is part of what was previously known as the selective androgen receptor degrader (SARD) program, in Oncternal’s reverse merger with GTx, Inc. in 2019. ONCT-534 has demonstrated preclinical activity in prostate cancer tumor models resistant to approved AR-targeting therapies. Oncternal is currently evaluating strategic development options for ONCT-534 as a potential therapy for castration-resistant prostate cancer (CRPC), LAR-TNBC as well as AR-driven non-oncology indications. 

Oncternal is currently seeking to amend the financial terms of a contingent value rights (CVR) agreement relating to the program, subject to approval of a majority in interest of the CVR holders. Among other things, the amendment would increase Oncternal’s share of proceeds from commercialization or other monetization of the program while limiting certain deductions in some cases to those costs incurred after the potential amendment becomes effective. Oncternal intends to provide a programmatic update on ONCT-534 on its earnings call planned for early November 2021.

About Oncternal Therapeutics (Nasdaq: ONCT)

Oncternal Therapeutics is a clinical-stage biopharmaceutical company focused on the development of novel oncology therapies for the treatment of cancers with critical unmet medical need. Oncternal focuses drug development on promising yet untapped biological pathways implicated in cancer generation or progression. The clinical pipeline includes cirmtuzumab, an investigational monoclonal antibody designed to inhibit the ROR1 pathway, a type I tyrosine kinase-like orphan receptor, that is being evaluated in a Phase 1/2 clinical trial in combination with ibrutinib for the treatment of patients with mantle cell lymphoma (MCL) and chronic lymphocytic leukemia (CLL) and in an investigator-sponsored, Phase 1b clinical trial in combination with paclitaxel for the treatment of women with HER2-negative metastatic or locally advanced, unresectable breast cancer, as well as a Phase 2 clinical trial of cirmtuzumab in combination with venetoclax, a Bcl-2 inhibitor, in patients with relapsed/refractory CLL. Oncternal is also developing a chimeric antigen receptor T cell (CAR-T) therapy that targets ROR1, which is currently in preclinical development as a potential treatment for hematologic cancers and solid tumors. The clinical pipeline also includes TK216, an investigational targeted small-molecule inhibitor of the ETS family of oncoproteins, that is being evaluated in a Phase 1/2 clinical trial for patients with Ewing sarcoma alone and in combination with vincristine chemotherapy. More information is available at https://oncternal.com.

SOURCE: Oncternal Therapeutics