abiraterone decanoate (ASP5541) / Astellas - LARVOL DELTA

Phase 2 study of ASP5541 (PRL-02), a long-acting intramuscular depot injection of abiraterone decanoate, in patients with advanced prostate cancer. (ASCO-GU 2026) - P1, P2 | "Recruitment is planned across the Americas, Europe, and the Asia-Pacific region. ASP5541 1260 mg IM once every 12 weeks (Q12W); AA 1000 mg orally (PO) once daily (QD); pred PO 5 mg twice daily for mCRPC and 5 mg QD for mHSPC."

Clinical • Metastases • P2 data • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Phase I trial of ASP5541 (PRL-02), a long-acting intramuscular depot injection of abiraterone decanoate, in patients (Pts) with advanced prostate cancer (PC) (ESMO 2025) - P1 | "Conclusions ASP5541 was well-tolerated, had low rates of mineralocorticoid toxicity, and showed antitumor activity in ARPI-naïve pts with mCRPC. ASP5541 will be further evaluated in a phase 2 study ± concomitant glucocorticoids."

Clinical • Metastases • P1 data • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

5541-CL-0201: A Phase 2 Study to Evaluate the Effects of ASP5541 in Participants with Prostate Cancer (clinicaltrialsregister.eu) - P1/2 | N=89 | Recruiting | Sponsor: Astellas Pharma Global Development Inc.

New P1/2 trial • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

A Study to Evaluate the Safety and Drug Levels of ASP5541 in Chinese Participants With Prostate Cancer (clinicaltrials.gov) - P1 | N=12 | Recruiting | Sponsor: Astellas Pharma Global Development, Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Hormone Sensitive Prostate Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

A Study to Evaluate the Safety and Drug Levels of ASP5541 in Chinese Participants With Prostate Cancer (clinicaltrials.gov) - P1 | N=12 | Not yet recruiting | Sponsor: Astellas Pharma Global Development, Inc.

New P1 trial • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Hormone Sensitive Prostate Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

Preclinical pharmacokinetic and pharmacodynamic study of GS24-B039, a 3-month long-acting abiraterone prodrug (ESMO 2025) - "The exposure of abiraterone after a single IM injection of GS24-B039 was 2.96-fold higher than that of AD (PRL-02, the first long-acting abiraterone prodrug in clinical trials) in the same vehicle. Legal entity responsible for the study Changchun GeneScience Pharmaceutical Co., Ltd. Funding Changchun GeneScience Pharmaceutical Co., Ltd."

PK/PD data • Preclinical • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

PRL-02-1001: A Safety and Dose-finding Study of PRL-02 Depot in Men With Advanced Prostate Cancer (clinicaltrials.gov) - P1 | N=174 | Recruiting | Sponsor: Astellas Pharma Global Development, Inc. | Trial primary completion date: Aug 2025 ➔ May 2029

Trial primary completion date • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Hormone Sensitive Prostate Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

A Phase 2 Study to Evaluate the Effects of ASP5541 in Participants With Prostate Cancer (clinicaltrials.gov) - P2 | N=218 | Recruiting | Sponsor: Astellas Pharma Global Development, Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Hormone Sensitive Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor

A Phase 2 Study to Evaluate the Effects of ASP5541 in Participants With Prostate Cancer (clinicaltrials.gov) - P2 | N=218 | Not yet recruiting | Sponsor: Astellas Pharma Global Development, Inc.

New P2 trial • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Hormone Sensitive Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor

PRL-02-1001: A Safety and Dose-finding Study of PRL-02 Depot in Men With Advanced Prostate Cancer (clinicaltrials.gov) - P1 | N=174 | Recruiting | Sponsor: Astellas Pharma Global Development, Inc. | Trial completion date: Apr 2025 ➔ May 2029 | Trial primary completion date: Dec 2024 ➔ Aug 2025

Metastases • Trial completion date • Trial primary completion date • Castration-Resistant Prostate Cancer • Castration-Sensitive Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

Abiraterone Decanoate (PRL-02/ASP5541): A Precision Approach to Androgen Biosynthesis Inhibition (PCF 2024) - No abstract available

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

PRL-02-1001: A Safety and Dose-finding Study of PRL-02 Depot in Men With Advanced Prostate Cancer (clinicaltrials.gov) - P1 | N=174 | Recruiting | Sponsor: Astellas Pharma Global Development, Inc. | Phase classification: P1/2 ➔ P1 | N=100 ➔ 174

Enrollment change • Metastases • Phase classification • Genito-urinary Cancer • Metastatic Castration-Resistant Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor

PRL-02-1001: Open-label, Multicenter Study of Intramuscular PRL-02 Depot in Patients With Advanced Prostate Cancer (clinicaltrials.gov) - P1/2 | N=100 | Recruiting | Sponsor: Propella Therapeutics | Trial primary completion date: Dec 2023 ➔ Dec 2024

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

Phase 1/2a study of PRL-02, a long-acting IM depot injection of abiraterone decanoate, in patients with prostate cancer including those previously treated with enzalutamide. (ASCO-GU 2024) - P1/2 | "PRL-02 was well tolerated. The RP2D of 1260 mg was selected over 1800 mg due to the absence of progesterone rises at 1260 mg. PRL-02 produces durable dose dependent T suppression and associated PSA response."

Clinical • P1/2 data • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Metastatic Castration-Resistant Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor

Astellas Completes Acquisition of Propella Therapeutics (PRNewswire) - "Astellas Pharma...announced today that it has completed the acquisition of Propella Therapeutics...and has become a wholly owned subsidiary of Astellas as of U.S. Eastern Time December 21, 2023. Through the acquisition of Propella, Astellas has acquired PRL-02 (abiraterone decanoate), a next-generation androgen biosynthesis inhibitor being developed by Propella to treat prostate cancer....PRL-02 is currently in a Phase 1 clinical trial and is expected to enter Phase 2a clinical trials in 2024. Under the agreement, Astellas paid approximately US $175 million to acquire all of the outstanding common stock and equity interests in Propella."

M&A • New P2a trial • Prostate Cancer

Astellas to Acquire Propella Therapeutics (Astellas Press Release) - "Astellas Pharma...and Propella Therapeutics...announced that Astellas, through a U.S. subsidiary, and Propella have entered into a merger agreement pursuant to which Astellas will acquire Propella. Propella is a privately held biopharmaceutical company that has leveraged a wholly owned proprietary platform that combines medicinal chemistry with lymphatic targeting to create new oncology drugs....Through the acquisition of Propella, Astellas will acquire PRL-02 (abiraterone decanoate), a next-generation androgen biosynthesis inhibitor being developed by Propella to treat prostate cancer....PRL-02 is currently in a Phase 1 clinical trial and is expected to enter Phase 2a clinical trials in 2024."

M&A • New P2a trial • Prostate Cancer

Phase 1/2a study of PRL-02, a long-acting intramuscular (IM) depot injection of abiraterone decanoate, in patients (pts) with advanced prostate cancer. (ASCO 2023) - P1/2 | "Only minimal and transient changes in ‘upstream’ steroids (e.g., progesterone) were observed at doses of 1260 mg (the RP2D) and lower. Clinical trial information: Clinical Trial information: NCT04729114. >"

Clinical • Metastases • P1/2 data • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • CYP17A1

Phase 1/2a study of PRL-02, a long-acting intramuscular (IM) depot injection of abiraterone decanoate in patients (pts) with advanced prostate cancer. (ASCO-GU 2023) - P1/2 | "PRL-02 was well tolerated. Dose-dependent T suppression was associated with clinical benefit including PSA responses and radiographic improvement. Based on a historical comparison, the levels of P and C are significantly lower than seen with AA + prednisone which appear to be due to greater CYP17 lyase selectivity."

Clinical • Metastases • P1/2 data • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Abiraterone decanoate (PRL-02): Pharmacology of a single intramuscular (IM) depot injection compared to oral abiraterone acetate (AA) in intact male rats. (ASCO-GU 2022) - P1/2 | "Single-dose IM PRL-02 blocked testicular CYP17 enzyme activity as effectively as daily AA in intact male rats and produced a durable large reduction in plasma T. The pharmacological activity, tissue and plasma distribution of TAE from IM PRL-02 in the rat model, along with results from prior monkey model studies, suggest the potential for a greater therapeutic index than from daily oral AA and support the ongoing evaluation of IM PRL-02 in patients with advanced prostate cancer."

Preclinical • Genito-urinary Cancer • Prostate Cancer • CYP17A1

Propella Therapeutics Announces Presentation of Updated Phase 1/2a Data of PRL-02 for the Treatment of Advanced Prostate Cancer at 2023 ASCO Genitourinary (GU) Cancers Symposium (GlobeNewswire) - "'The PRL-02 Phase 1 data suggest both clinical efficacy advantages as well as safety and tolerability benefits for advanced prostate cancer patients who may have received approved androgen receptor inhibitor therapy,' said Neal Shore, MD, FACS...'I am very encouraged by the emerging PRL-02 profile and its clinically meaningful potential which could broaden our current armamentarium for patients with metastatic prostate cancer.'"

Media quote

Propella Therapeutics Announces Presentation of Updated Phase 1/2a Data of PRL-02 for the Treatment of Advanced Prostate Cancer at 2023 ASCO Genitourinary (GU) Cancers Symposium (GlobeNewswire) - "Separately, Propella also announced the United States Patent and Trademark Office (USPTO) issued U.S. Patent No. 11,559,534, titled 'Abiraterone Prodrugs,' on January 24, 2023. The ‘534 patent protects the abiraterone decanoate compound and its related pharmaceutical compositions, unit dosage forms comprising abiraterone decanoate, and methods of treating prostate cancer with pharmaceutical compositions comprising abiraterone decanoate. The ‘534 patent also discloses related methods of treating other androgen-dependent disorders, combination therapies, methods of reducing serum testosterone using a pharmaceutical composition comprising a lipophilic abiraterone prodrug. The ‘534 expires on March 4, 2040."

Patent • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Propella Therapeutics Announces Presentation of Updated Phase 1/2a Data of PRL-02 for the Treatment of Advanced Prostate Cancer at 2023 ASCO Genitourinary (GU) Cancers Symposium (GlobeNewswire) - P1/2 | N=100 | NCT04729114 | Sponsor: Propella Therapeutics | "Propella Therapeutics...announced that Dr. Jose Avitia of the New Mexico Cancer Center will present updated data from the Company’s ongoing Phase 1/2a study of PRL-02 for the treatment of advanced prostate cancer on Thursday Feb 16 from 11:30AM to 1:00PM PST at the 2023 ASCO Genitourinary (GU) Cancers Symposium....The presentation will highlight results from the ongoing dose-escalation part of the Phase 1/2 study (NCT04729114). At the time of abstract submission, safety, tolerability and activity results were available from 17 patients who had been treated at five different dose levels of PRL-02 (180mg; 360mg; 720mg; 1260mg; 1800mg). PRL-02, administered as an intramuscular injection every 12 weeks, was well tolerated; dose-dependent androgen suppression was associated with clinical benefit including PSA responses and radiographic improvement."

P1/2 data • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

1/2a study of PRL-02, a long-acting IM depot injection of abiraterone decanoate in patients with prostate cancer (NCT04729114) (ESMO 2022) - P1/2 | "Dose dependent T suppression associated with clinical benefit (PSA response / radiographic improvement) was observed. The study continues."

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

Propella Therapeutics Announces Presentation of Phase 1/2 Data of PRL-02 for the Treatment of Advanced Prostate Cancer at ESMO Congress 2022 (GlobeNewswire) - "Propella Therapeutics...announced that Dr. Jose Avitia of the New Mexico Cancer Center will present data from the Company’s ongoing Phase 1/2 trial of PRL-02 for the treatment of advanced prostate cancer on Sunday, September 11 at 12:00 pm at the European Society for Medical Oncology (ESMO) Congress 2022....The presentation will highlight results from the ongoing dose-escalation part of the Phase 1/2 study (NCT04729114) in 15 patients who have been treated at five different doses of PRL-02 (180mg; 360mg; 720mg; 1260mg; 1800mg), including safety, tolerability and response data."

P1/2 data • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

PRL-02-1001: Open-label, Multicenter Study of Intramuscular PRL-02 Depot in Patients With Advanced Prostate Cancer (clinicaltrials.gov) - P1/2 | N=100 | Recruiting | Sponsor: Propella Therapeutics | N=33 ➔ 100 | Trial completion date: Dec 2023 ➔ Apr 2025

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