Sponsor Decision

This is a Phase 1, open-label study that will evaluate the safety and tolerability of FT-7051 and determine the recommended Phase 2 dose (RP2D) as well as pharmacokinetics (PK), preliminary anti-tumor activity, and pharmacodynamics (PD) of FT-7051 in men with metastatic castration-resistant prostate cancer who have progressed despite prior therapy and had been treated with at least one potent anti-androgen therapy.

The starting dose, 25 mg once daily (QD), of FT-7051 administered discontinuously (21 days on/7 days off) in 28-day cycles.

Inclusion Criteria:

• Signed informed consent
• Diagnosis of progressive metastatic castration-resistant prostate cancer (mCRPC)
• Previously failed at least one potent anti-androgen therapy
• Castrate levels of serum testosterone
• ECOG performance status 0-2
• Adequate bone marrow function
• Adequate kidney, heart and liver function

Exclusion Criteria:

• Prior solid organ transplant
• Prior treatment with small molecules including chemotherapy, antibody, or other experimental anticancer therapeutic within 4 weeks of first dose of study treatment
• Prior radiation therapy within 4 weeks prior to initiation of study treatment (including radiofrequency ablation)
• Prior androgen antagonist therapy (enzalutamide, apalutamide, abiraterone acetate, or darolutamide) within 2 weeks
• Prior radium-223 therapy within 6 weeks
• Symptomatic, untreated or actively progressing central nervous system (CNS) metastasis
• Unstable or severe, uncontrolled medical condition (e.g., unstable cardiac function, unstable pulmonary condition including pneumonitis and/or interstitial lung disease, uncontrolled diabetes, active or uncontrolled infection requiring systemic therapy) or any important medical illness or abnormal laboratory finding that would, in the Investigator's judgement, increase the risk to the patient associated with participation in the study
• Concomitant medications that cause Torsades de Pointes that have not reached steady state before first dose of the study drug
• Concomitant medications that are strong inhibitors or inducers of CYP3A4 or an inhibitor of P-gp
• History of infection with human immunodeficiency virus (HIV)
• Active infection with hepatitis B, or hepatitis C virus