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A Phase I/II Study to Assess the Safety, Pharmacokinetics, and Anti-Tumor Activity of Oral HP518 in mCRPC Patients

Phase 1
Recruiting
Conditions
Metastatic Castration-resistant Prostate Cancer
Interventions
Drug: HP518 - Dose Escalation
Drug: HP518 -Dose Expansion
Registration Number
NCT06155084
Lead Sponsor
Hinova Pharmaceuticals Inc.
Brief Summary

The overall objective of this Phase 1 study is to evaluate the safety, PK,and anti-tumor activity of daily oral dosing with HP518,selecting the RP2D of HP518 based on assessments of patients with progressive mCRPC in dose-escalation phase

Detailed Description

This First in Human dose escalation and expansion study of HP518 in patients with progressive mCRPC after NHA and chemotherapy is being conducted not only to evaluate the safety and tolerability of orally administered HP518, but also to provide preliminary efficacy for the reference of future studies.

Recruitment & Eligibility

Status
RECRUITING
Sex
Male
Target Recruitment
84
Inclusion Criteria
  1. Male, age ≥18
  2. Patients with androgen receptor (AR) ligand binding domain (LBD) activation mutations (the dose expansion part of stage II)
  3. Has histologically confirmed adenocarcinoma of the prostate, but there are no known significant neuroendocrine differentiation or small cell characteristics.
  4. Has metastatic disease documented by 2 or more bone lesions by bone scan or soft tissue disease progression observed by CT/MRI at the beginning of study.
  5. the progression of the disease after receiving at least one new endocrine therapy and progressing with at least first-line chemotherapy.
  6. Must have recovered from toxicities related to any prior treatments
  7. Ongoing ADT with LHRH agonist/antagonist therapy or history of bilateral orchiectomy.
  8. ECOG performance status score of 0 to 1.
Exclusion Criteria
  1. Combination of research or commercially available drugs targeting AR
  2. Has had any other anticancer treatments, including immunotherapy, chemotherapy, or radiotherapy (eg, 177LuPSMA-617, radium 223, PARP inhibitor) within 4 weeks prior to the first dose of HP518.
  3. Has gastrointestinal disorder affecting absorption (e.g., gastrectomy).
  4. Has significant cardiovascular disease.

Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
Part 1 - Dose Escalation, 400mg/d (Cohort1)HP518 - Dose EscalationOral tablet(s), once daily in 28-day cycles
Part 1 - Dose Escalation 500mg/d (Cohort 2)HP518 - Dose EscalationOral tablet(s), once daily in 28-day cycles
Part 2 - Dose Expansion Oral tablet(s)HP518 -Dose ExpansionOral tablet(s), once daily in 28-day cycles
Primary Outcome Measures
NameTimeMethod
Incidence of vital signs abnormalities characterized by type, frequency, severity (as graded by NCI CTCAE version 5.0), and timingThrough study completion, an average of 1 year

To evaluate the safety of orally administered HP518 (Part 1)

Incidences of Protocol-defined DLT during the DLT assessment period , characterized by type, frequency, severity (as graded by NCI CTCAE version 5.0), timing, seriousness, and relationship to study drugorally administered HP518 (Part 1)28 DAYS

To evaluate the safety and tolerability and determine the MTD and the RP2D of orally administered HP518 (Part 1)

Incidence of Treatment-Emergent Adverse Events characterized by type, frequency, severity (as graded by NCI CTCAE version 5.0), timing, seriousnessThrough study completion, an average of 1 year

To evaluate the safety of orally administered HP518 (Part 1)

Incidence of ECG (PR, QRS, QT, and QTcF intervals) abnormalities characterized by type, frequency, severity (as graded by NCI CTCAE version 5.0), and timingThrough study completion, an average of 1 year

To evaluate the safety of orally administered HP518 (Part 1)

PSA50 response rate12 weeks

Proportion of patients showing a PSA decline by ≥50% between baseline and Week 12 of dosing with HP518.

Incidence of laboratory abnormalities, characterized by type, frequency, severity (as graded by NCI CTCAE version 5.0), and timingThrough study completion, an average of 1 year

To evaluate the safety of orally administered HP518 (Part 1)

Secondary Outcome Measures
NameTimeMethod
Apparent terminal elimination half-life (T1/2)12 weeks

Assessment of pharmacokinetic parameters of HP518

apparent volume of distribution during the terminal phase after extravascular administration (Vz/F)12 weeks

Assessment of pharmacokinetic parameters of HP518

oral clearance (CL/F)12 weeks

Assessment of pharmacokinetic parameters of HP518

According to PCWG38 weeks

evaluate PSA50 response rate: PSA decline by≥50% between baseline and 4 weeks/8 weeks/12 weeks( only Part 1) of dosing with HP518

According to PCWG3, evaluate time to PSA progressionThrough study completion, an average of 1 year

PCWG3 definition: PSA increase \>25% and \>2 ng/mL above nadir, confirmed by progression at 2 time points at least 3 weeks apart) nadir, confirmed by progression at 2 time points at least 3 weeks apart)

area under the concentration-time curve (AUC)12 weeks

Assessment of pharmacokinetic parameters of HP518

Maximum concentration (Cmax)12 weeks

Assessment of pharmacokinetic parameters of HP518

Time to maximum concentration (Tmax)12 weeks

Assessment of pharmacokinetic parameters of HP518

Time to radiographic progression by investigator PCWG3 definitionThrough study completion, an average of 1 year

using the RECIST v1.1 and PCWG3 definition

Evaluate the modified best overall response mBOR by investigatorThrough study completion, an average of 1 year

According to RECIST (version 1.1) and PCWG3

analyze the efficacy of patients with different AR phenotypes(Part 2)Through study completion, an average of 1 year

According to genetic testing results

Trial Locations

Locations (27)

The Second Hospital Of Anhui Medical University

🇨🇳

Hefei, Anhui, China

Beijing Friendship Hospital, Capital Medical University

🇨🇳

Beijing, Beijing, China

Chongqing University Cancer Hospital

🇨🇳

Chongqing, Chongqing, China

The Second Affiliated Hospital Of Chongqing Medical University

🇨🇳

Chongqing, Chongqing, China

The First Affiliated Hospital Of Xiamen Univeristy

🇨🇳

Xiamen, Fujian, China

Lanzhou University Second Hospital

🇨🇳

Lanzhou, Gansu, China

The Third Affiliated Hospital of Southern Medical University

🇨🇳

Guangzhou, Guangdong, China

The Affiliated Hospital Of Guizhou Medical University

🇨🇳

Guiyang, Guizhou, China

Henan Cancer Hospital

🇨🇳

Zhengzhou, Henan, China

Zhengzhou Central Hospital

🇨🇳

Zhengzhou, Henan, China

Tongji Hospital

🇨🇳

Wuhan, Hubei, China

Hunan Cancer Hospital

🇨🇳

Changsha, Hunan, China

The First Affiliated Hospital Of Nanchang University

🇨🇳

Nanchang, Jiangxi, China

Liaoning Cancer Hospital & Institute

🇨🇳

Shenyang, Liaoning, China

Shandong Provincial Hospital

🇨🇳

Jinan, Shandong, China

The Affiliated Hospital Of Qingdao University

🇨🇳

Qingdao, Shandong, China

Yantai Yuhuangding Hospital

🇨🇳

Yantai, Shandong, China

Shanghai Tenth People's Hospital

🇨🇳

Shanghai, Shanghai, China

The First Affiliated Hospital Of Xi'An Jiaotong Univeristy

🇨🇳

Xi'An, Shanxi, China

Sichuan Academy of Medical Science & Sichuan Provincial People's Hospital

🇨🇳

Chengdu, Sichuan, China

West China Hospital Of Sichuan University

🇨🇳

Chengdu, Sichuan, China

The Affiliated Hospital Of Southwest Medical University

🇨🇳

Luzhou, Sichuan, China

Mianyang Central Hospital

🇨🇳

Mianyang, Sichuan, China

The Second Affiliated Hospital Of Kunming Medical University

🇨🇳

Kunming, Yunnan, China

The Affiliated Hospital Of School Of Medicine Of Ningbo University

🇨🇳

Ningbo, Zhejiang, China

The First Affiliated Hospital of Wenzhou Medical University

🇨🇳

Wenzhou, Zhejiang, China

Beijing Cancer Hospital

🇨🇳

Beijing, Beijing, China

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