Tas::75 0849::Tas Topic 255: a Novel; Non-Competitive Androgen Receptor Inhibito
Award last edited on: 1/8/2024

Sponsored Program
Awarding Agency
Total Award Amount
Award Phase
Solicitation Topic Code
Principal Investigator
Brent Blackburn

Company Information

Arta Bioscience Inc

54 Aberdeen Place
Saint Louis, MO 63105
   (415) 533-7450
Location: Single
Congr. District: 02
County: St. Louis

Phase I

Contract Number: 261201100095C-0-0-1
Start Date: 9/30/2011    Completed: 7/29/2012
Phase I year
Phase I Amount
The androgen receptor (AR) remains a key therapeutic target for prostate cancer (PCa), even in castration resistant PCa (CRPC). Current therapies target AR by blocking androgen synthesis or competitive antagonism. ARTA Bioscience is developing an early lead, ABS-001, a non-competitive AR inhibitor that is synergistic with competitive antagonists. It blocks ligand-induced conformational change in AR at nanomolar levels in vitro and in vivo, without affecting hormone binding. It is effective against constitutively active AR truncation products that may playa role in CRPC, and AR mutants with reduced sensitivity to competitive antagonists. It has the potential to complement, if not supplant, all existing anti-androgen therapies used for CRPC, and might also be extended as a first line therapy. The grant has three objectives. 1 ) Chemically characterize ABS-001 to determine the activity of each enantiomer; determine solubility and optimal formulation parameters; carry out early pharmacokinetic studies in rodents. 2) Carry out pharmacodynamic studies in rodents to confirm AR inhibitory activity in wild-type mice, and xenograft models of prostate cancer. 3) Characterize ABS-001 in vitro using standard measures of potential cardiotoxicity and mutagenicity. If successful, this compound will be ready for IND-enabling studies to be funded by a Phase II SBIR grant.

NIH Spending Category:
Cancer; Prostate Cancer; Urologic Diseases

Project Terms:
Affect; Androgen Receptor; Androgens; Antiandrogen Therapy; Bicalutamide; Binding (Molecular Function); bone; Brain; Cardiotoxicity; Castration; Complement; Contracts; cost; Data; Dose; Drug Formulations; Drug Kinetics; enantiomer; Exhibits; Funding; Gene Activation; Gene Expression; Goals; Grant; Harvest; Hormones; Human; In Vitro; in vivo; Industry; inhibitor/antagonist; Investments; Lead; Ligands; Liver; male; Malignant neoplasm of prostate; Metabolic; Mus; Muscle; mutant; novel; Pharmaceutical Chemistry; Pharmacodynamics; Phase; Prostate; Receptor Cell; Relative (related person); Repression; Research Contracts; Resistance; RNA; Rodent; Role; Skeletal muscle structure; Small Business Innovation Research Grant; Solubility; standard measure; Supplementation; Testing; therapeutic target; therapy design; Tissues; Toxic effect; tumor growth; Wild Type Mouse; Xenograft Model

Phase II

Contract Number: ----------
Start Date: 00/00/00    Completed: 00/00/00
Phase II year
Phase II Amount