CBP-1018 / Coherent Biopharma - LARVOL DELTA

Updated results from a phase I/II study of CBP-1018, a bi-ligand–drug conjugate (Bi-XDC) as late line therapy for patients with metastatic castration resistant prostate cancer (mCRPC). (ASCO-GU 2025) - P1 | "CBP-1018 shows potential as a viable therapeutic option for heavily treated mCRPC pts based on the superior rPFS and anti-tumor activity, warranting further evaluation in later phase III trials."

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

CBP-1018, Bi-ligand-drug conjugate (Bi-XDC) drug treated for metastatic castration resistant prostate cancer (mCRPC) patients from phase I study results (ESMO 2024) - P1 | "CBP-1018, as the first bi-XDC globally, has showed a promising preliminary efficacy and well-tolerated safety profile in mCRPC pts, supporting a further investigation in mCRPC pts to decide optimal dose and further confirmation in a large scale population. Yehui Shi and Hai Huang are the corresponding authors."

Clinical • Metastases • P1 data • Genito-urinary Cancer • Metastatic Castration-Resistant Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor • FOLR1

A Study of CBP-1018 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=170 | Recruiting | Sponsor: Coherent Biopharma (Suzhou) Co., Ltd. | Trial primary completion date: Dec 2023 ➔ Oct 2024

Metastases • Trial primary completion date • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Prostate Cancer • Renal Cell Carcinoma • Solid Tumor • FOLR1

LC-MS/MS method for dual-ligand peptide-drug CBP-1018 and its deconjugated payload MMAE including sample stabilization strategy for its MC-Val-Cit-PABC linker. (PubMed, Talanta) - "The results showed that CBP-1018 was eliminated immediately after injection and MMAE reached the maximum exposure at approximately 2 h after infusion. The maximum concentration of MMAE did not exceed 20.0 ng/mL, suggesting that the off-target toxicity of CBP-1018 injection was controllable."

Journal • Oncology • Solid Tumor • CTSS

A phase 1, multi-center, open-label, dose-escalation, and dose-expansion study of CBP-1018, a bi-ligand-drug conjugate in patients with heavily treated advanced solid tumors. (ASCO 2024) - P1 | "CBP-1018 was well-tolerated at DLs of 0.03-0.16 mg/kg Q2W with no DLTs. MTD was not reached. Promising preliminary efficacy ORR and rPFS were observed, supporting a further investigation in large scale clinical trial for mCRPC patients."

Clinical • Metastases • P1 data • Bladder Cancer • Breast Cancer • Gastrointestinal Cancer • Genito-urinary Cancer • Hepatology • Lung Cancer • Metastatic Castration-Resistant Prostate Cancer • Oncology • Ovarian Cancer • Pancreatic Cancer • Prostate Cancer • Solid Tumor • FOLR1

CBP-1018, a dual-ligand drug targeting PSMA-FOLR1, is available for prostate cancer treatment and has the potential to be used in combination with other therapies (AUA 2024) - "Our results demonstrated that CBP-1018 is a dual-targeted ligand drug that can be used in prostate cancer treatment, has significant ex vivo and ex vivo anti-tumor effects, and can be combined with other prostate cancer therapeutic agents to produce stronger anti-tumor effects, which provides a new drug option and therapeutic strategy for the treatment of prostate cancer."

Combination therapy • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • FOLR1 • PSMA1

CBP-8008: A first-in-class targeted pan-Bet protein degradation therapy using bi-specific XDC (Bi-XDC) technology for TNBC and mCRPC (AACR 2024) - "Several anticancer Bi-ligand drug conjugates including CBP-1008, CBP-1018, and CBP-1019 have been brought into various clinical stages in China and US. CBP-8008 is currently in preclinical development as a potential first-in-class pan-Bet protein degradation therapy using Bi-XDC technology for TNBC and mCRPC"

Breast Cancer • Metastatic Castration-Resistant Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor • Triple Negative Breast Cancer • BRD2 • BRD3 • BRD4 • FOLR1

CBP-1018, a bi-ligand-drug conjugate treated in patients with advanced solid tumors: A phase I, multi-center, open-label, dose-escalation and dose expansion study (ESMO 2023) - P1 | "Multiple SD and PSA decrease were observed at DLs of 0.08-0.14 mg/kg, conferred a promising preliminary antitumor activity in pts with mCRPC despite of COVID-19's impacts. MTD was not reached and dose-escalation to establish the RP2D is continuing."

Clinical • Metastases • Bladder Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • FOLR1

Bispecific-XDC: Novel First-in-Class Cancer Therapies From Concept to Clinical (ADC-USA 2023) - "Describing CBP-1008: a FR/ TRPV6 targeted drug conjugate in Phase II pivotal studies of advanced ovarian cancer treatment; Exploring CBP-1018: a FR/ PSMA targeted drug conjugate in Phase Ib for prostate cancer therapy; Highlighting CBP-1019: TOP1i payload drug conjugate for unmet medical needs"

Clinical • Genito-urinary Cancer • Oncology • Ovarian Cancer • Prostate Cancer • Solid Tumor • TRPV6

A phase 1, multi-center, open-label, dose-escalation and dose expansion study of CBP-1018, a bi-ligand-drug conjugate, in patients with heavily treated advanced solid tumors. (ASCO 2023) - P1 | "CBP-1018 was well-tolerated at DLs of 0.03-0.12 mg/kg Q2W with no DLTs. Multiple SD were observed at DLs of 0.08-0.12 mg/kg, conferred a promising preliminary antitumor activity in pts with mCRPC. MTD was not reached and dose-escalation to establish the RP2D is continuing."

Clinical • Metastases • P1 data • Bladder Cancer • Dyslipidemia • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • Urothelial Cancer • FOLH1 • FOLR1

A Study of CBP-1018 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=170 | Recruiting | Sponsor: Coherent Biopharma (Suzhou) Co., Ltd. | Not yet recruiting ➔ Recruiting | Trial completion date: Oct 2023 ➔ Oct 2024 | Trial primary completion date: Oct 2022 ➔ Dec 2023

Enrollment open • Metastases • Trial completion date • Trial primary completion date • Non Small Cell Lung Cancer • Oncology • Prostate Cancer • Renal Cell Carcinoma • Solid Tumor

Bispecific XDC – A Versatile Drug Delivery Platform (ADC London 2023) - "Synopsis Design and mechanism of Bi-XDC: Leveraging bi-ligand synergies on multiple dimensions to drug the undruggable targets and pipeline of Bi- XDC platform Clinical Progress of CBP- 1008 and CBP-1018"

An open-label, non-randomized, multi-center phase I study evaluating the safety, tolerability, pharmacokinetics and preliminary efficacy of bi-ligand-drug conjugate CBP-1018 in patients with advanced solid tumors. (ASCO 2022) - P1 | "Enrollment has been started in Nov. 2021 and is ongoing."

Clinical • P1 data • PK/PD data • Genito-urinary Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Prostate Cancer • Renal Cell Carcinoma • Solid Tumor • Squamous Cell Carcinoma • FOLR1

A Study of CBP-1018 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1; N=170; Not yet recruiting; Sponsor: Coherent Biopharma (Suzhou) Co., Ltd.

New P1 trial • Non Small Cell Lung Cancer • Oncology • Renal Cell Carcinoma • Solid Tumor