Phase 1 Study of ACE-232 to Treat Patients With Metastatic Castration-Resistant Prostate Cancer

A Phase 1 Study to Assess the Safety, Pharmacokinetics, Pharmacodynamics, and Preliminary Efficacy of ACE-232 in Patients With Metastatic Castration-Resistant Prostate Cancer (CRPC)

This is an open label, phase I, multi-center study aiming to assess the safety and tolerability in patients with metastatic castration resistant prostate cancer (mCRPC).

Study Overview

• Status: Recruiting
• Conditions: Prostate Cancer (Adenocarcinoma); mCRPC (Metastatic Castration-resistant Prostate Cancer)
• Intervention / Treatment: Drug: ACE-232 tablets

Detailed Description

The study consists of two parts, Phase 1A dose escalation and Phase 1B dose optimization. Phase 1A aims to assess the safety, tolerability, pharmacokinetic (PK) profile, and changes in pharmacodynamic (PD) markers in patients treated with ACE-232, and to determine the maximum tolerated dose (MTD), if applicable. In Phase 1B, patients with AR gene alterations will be treated at two different dose levels to establish the recommended Phase 2 dose (RP2D).

• Study Type: Interventional
• Enrollment (Estimated): 67
• Phase: Phase 1

Contacts and Locations

• Study Contact: Name: Sherwin Cai, MD; Phone Number: 86-18983021726; Email: sherwin.cai@acerand.com
• Study Contact Backup: Name: Teresa Shi, MS; Phone Number: 86-13916513539; Email: teresa.shi@acerand.com

Study Locations

• United States
  • California
    • La Jolla, California, United States, 92093
      • Recruiting
      • University of California San Diego, Moores Cancer Center
  • Florida
    • Tampa, Florida, United States, 33612
      • Recruiting
      • Moffitt Cancer Center, Tampa
  • Maryland
    • Baltimore, Maryland, United States, 21201
      • Recruiting
      • University of Maryland, Greenebaum Comprehensive Cancer Center
  • Massachusetts
    • Boston, Massachusetts, United States, 02114
      • Recruiting
      • Harvard Medical School-Massachusetts General Hospital
  • Minnesota
    • Minneapolis, Minnesota, United States, 55455
      • Recruiting
      • M Health Fairview Clinics and Surgery Center
  • Nebraska
    • Omaha, Nebraska, United States, 68130
      • Recruiting
      • Xcancer (Urology Cancer Center)
  • South Carolina
    • Myrtle Beach, South Carolina, United States, 29572
      • Recruiting
      • Carolina Urologic Research Center
  • Washington
    • Seattle, Washington, United States, 98109
      • Recruiting
      • Fred Hutchinson Cancer Research Center

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: Adult; Older Adult
• Accepts Healthy Volunteers: No

Description

Inclusion Criteria:

• Provide written informed consent
• Metastatic Castration-resistant Prostate Cancer with ongoing androgen - deprivation therapy (ADT) or have bilateral orchiectomy
• Difficult to treat or intolerant to standard treatment (post at least 1 line of NHA and taxane-based chemo in mHSPC or mCRPC), suitable for investigational treatment;
• Has Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1
• Has a life expectancy of at least 6 months
• Adequate organ function and bone marrow function

Exclusion Criteria:

• Receiving any anti-cancer drugs or other treatment, major surgery, extensive radiation therapy, or local radiation therapy within protocol-defined wash-out period;
• Concomitant use of medications or herbal supplements known to be moderate to strong CYP3A4 inhibitors/inducers, or P-gp inhibitors, known to prolong the QT interval.
• Any previous treatment-related toxicities have not recovered.
• Spinal cord compression or known brain metastases or leptomeningeal carcinomatosis.
• Severe cardiovascular disorders.
• Known gastrointestinal (GI) disorder or GI procedure
• History of gastric and duodenal perforation.
• History of pituitary dysfunction.
• Poorly controlled diabetes mellitus.
• Active or uncontrolled autoimmune disease
• Active infections, or a known history of HIV infection, or a known active hepatitis B or C, or a known active tuberculosis.
• Other malignancies requiring treatment within 3 years prior to the first dose of study drug
• Known allergy or hypersensitivity to any of the excipients of ACE-232.
• Has other medical conditions that at the discretion of the investigator interfere with safety or efficacy evaluation, or treatment compliance.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: ACE-232	Drug: ACE-232 tablets; ACE-232 tablets will be administered orally daily as a continuous regimen together with Dexamethasone and Fludrocortisone. Subjects will continue to receive study treatment until PD as judged by local investigator review, development of unacceptable toxicity, or withdrawal of consent.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Number of patients experiencing adverse events (AEs)/serious adverse events (SAEs)	Number of patients with incidence of adverse events and with serious adverse events including changes from baseline in laboratory parameters, vital signs, ECGs, and physical examination, etc.	From time of information consent to 30 days post last dose, up to approximately 37 months
Number of patients experiencing dose limiting toxicity (DLT), as defined in the protocol	A DLT is defined as any toxicity events related to ACE-232 that occur from the first dose of study treatment until the planned end date of Cycle 1 (DLT assessment period), meeting the criteria specified in protocol.	From the first dose of ACE-232 on Cycle 1 Day 1 up to and including the planned end of Cycle 1 (at the end of 28 days)
Recommended Phase 2 dose (RP2D) and/or maximum tolerated dose (MTD)	RP2D will be finally determined by the SMC and sponsor based on all data from the dose escalation module and backfill module, as well as the exposure-response relationship evaluated (if available). MTD is defined as the maximum dose level at which ≤1 patient have DLTs during the DLT observation period, and it should be determined with 6 evaluable patients.	Up to approximately 37 months

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Pharmacokinetics characterization by using Area under the plasma concentration versus time curve (AUC)	To determine the pharmacokinetics (PK) using AUC of ACE-232 after a single dose and at steady state after multiple doses.	Up to approximately 37 months
Pharmacokinetics characterization by using Maximum concentration (Cmax)	To determine the pharmacokinetics (PK) using Cmax of ACE-232 after a single dose and at steady state after multiple doses	Up to approximately 37 months
Prostate Specific Antigen (PSA) response	PSA response is defined as PSA decline of 30% and 50% from baseline at any time point	Up to approximately 37 months
Objective Response Rate (ORR)	ORR is defined as a complete response (CR) or partial response (PR), as determined by the investigator using Response Evaluation Criteria in Solid Tumors (RECIST version 1.1) and Prostate Cancer Working Group Criteria 3 (PCWG3 criteria), in patients with measurable disease at baseline.	Up to approximately 37 months
Duration of Response (DoR)	DOR is defined, for patients with an objective response, as the time from first documentation of objective tumor response (CR or PR) to the first documentation of objective tumor progression or death due to any cause.	Up to approximately 37 months
Radiographic Progression Free Survival (rPFS)	rPFS is defined as the time from the first dose of ACE-232 to the first documented disease progression by either RECIST progression and/or progression on bone scan by PCWG3 or death due to any cause, whichever occurs first.	Up to approximately 37 months
Overall Survival (OS)	OS is defined as the time from the first dose of ACE-232 to the date of death due to any cause.	Up to approximately 37 months
Blood concentration of steroid hormone	To determine the blood concentration of steroid hormones at various timepoints and change from baseline	Up to approximately 37 months

Other Outcome Measures

Outcome Measure	Measure Description	Time Frame
Gene aberrations	To determine the gene aberrations in circulating tumor DNA (ctDNA), and its association with tumor response or resistance to ACE-232	Up to approximately 37 months

Collaborators and Investigators

• Sponsor: Acerand Therapeutics (Hong Kong) Limited

Study record dates

Study Major Dates

• Study Start (Actual): May 12, 2025
• Primary Completion (Estimated): March 1, 2028
• Study Completion (Estimated): August 1, 2028

Study Registration Dates

• First Submitted: January 19, 2025
• First Submitted That Met QC Criteria: January 24, 2025
• First Posted (Actual): January 30, 2025

Study Record Updates

• Last Update Posted (Actual): April 9, 2026
• Last Update Submitted That Met QC Criteria: April 8, 2026
• Last Verified: December 1, 2025

More Information

Terms related to this study

• Keywords: prostate cancer; Antineoplastic Agents; CRPC; Prostatic Neoplasms; castration-resistant prostate cancer; Hormone Antagonists; Hormone Substitutes; Castration-Resistant; ACE-232; CYP11A1
• Additional Relevant MeSH Terms: Urogenital Diseases; Genital Diseases; Genital Neoplasms, Male; Urogenital Neoplasms; Neoplasms by Site; Neoplasms; Genital Diseases, Male; Prostatic Diseases; Male Urogenital Diseases; Neoplasms by Histologic Type; Neoplasms, Glandular and Epithelial; Carcinoma; Prostatic Neoplasms; Adenocarcinoma
• Other Study ID Numbers: ACE-232-001

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO
• IPD Plan Description: No IPD sharing plan at this moment, which might be changed during the study process or when the results come out.

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: No