gunagratinib (ICP-192) / InnoCare - LARVOL DELTA

Metabolic stability assessment and metabolite profiling of gunagratinib, a novel FGFR inhibitor, in rat, monkey and human liver microsomes by an integrated analysis method based on HPLC-MS/MS and HPLC-Orbitrap-HRMS. (PubMed, J Pharm Biomed Anal) - "This study presents the first integrated analytical method based on HPLC-MS/MS and HPLC-Orbitrap-HRMS for the in vitro metabolic assessment of gunagratinib. We anticipate the clinical application of this method in future pharmacokinetic or metabolism studies."

Journal • Preclinical • Biliary Cancer • Cholangiocarcinoma • Head and Neck Cancer • Oncology • Solid Tumor • FGFR

Gunagratinib, a highly selective irreversible FGFR inhibitor in patients with head and neck cancer harboring FGFR pathway alterations (ESMO 2025) - P1/2, P2 | "Legal entity responsible for the study innocare Innocare. Funding innocare."

Clinical • Head and Neck Cancer • Nasopharyngeal Carcinoma • Oncology • Salivary Gland Cancer • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck • FGF3 • FGFR1

An Efficacy and Safety Study of ICP-192 in Subjects With Bladder Urothelial Cancer (clinicaltrials.gov) - P2 | N=115 | Recruiting | Sponsor: Beijing InnoCare Pharma Tech Co., Ltd. | Trial primary completion date: Feb 2024 ➔ Dec 2024

Metastases • Trial primary completion date • Bladder Cancer • Genito-urinary Cancer • Oncology • Solid Tumor • Urothelial Cancer

A Study of ICP-192 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1/2 | N=45 | Recruiting | Sponsor: Beijing InnoCare Pharma Tech Co., Ltd. | Trial completion date: Feb 2023 ➔ Apr 2024 | Trial primary completion date: Oct 2022 ➔ Nov 2023

Metastases • Trial completion date • Trial primary completion date • Biliary Cancer • Cholangiocarcinoma • Gastrointestinal Cancer • Oncology • Solid Tumor • Urothelial Cancer • FGFR

A Study of ICP-192 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1/2; N=45; Recruiting; Sponsor: Beijing InnoCare Pharma Tech Co., Ltd.; Initiation date: Sep 2020 ➔ Feb 2021

Clinical • Trial initiation date • Biliary Cancer • Cholangiocarcinoma • Gastrointestinal Cancer • Oncology • Solid Tumor • Urothelial Cancer • FGFR

Gunagratinib, a highly selective irreversible FGFR inhibitor, in patients with previously treated locally advanced or metastatic cholangiocarcinoma harboring FGFR pathway alterations: A phase IIa dose-expansion study. (ASCO-GI 2023) - P1/2 | "The study data demonstrated that gunagratinib is safe and well-tolerated in previously treated patients with locally advanced or metastatic CCA harboring FGFR2 gene fusions or rearrangements. The response rate in such a patient group is high comparing to other approved FGFR inhibitors. Gunagratinib is a promising second-generation FGFR inhibitor with potential for the treatment of multiple indications with FGF/FGFR pathway abnormalities."

Clinical • Metastases • P2a data • Biliary Cancer • Cholangiocarcinoma • Gastrointestinal Cancer • Oncology • Solid Tumor • FGFR2

Latest Clinical Data of InnoCare’s Gunagratinib Presented at 2023 ASCO GI (Businesswire) - P1/2 | N=59 | NCT03758664 | Sponsor: Beijing InnoCare Pharma Tech Co., Ltd. | "As of September 5, 2022, 18 cholangiocarcinoma patients were treated orally with gunagratinib 20 mg QD. The median age of the patients was 52 with 44.4% male. Among 17 patients who have completed at least one tumor assessment, the overall response rate (ORR) was 52.9%, the disease control rate (DCR) was 94.1% and median progression free survival (mPFS) was 6.93 months (not reached at cutoff). Gunagratinib showed a well-tolerated safety profile."

P2a data • Biliary Tract Cancer • Cholangiocarcinoma • Gastrointestinal Cancer • Oncology • Solid Tumor

A Study of ICP-192 in Patients With FGFR2-Rearranged Unresectable or Metastatic Intrahepatic Cholangiocarcinoma (clinicaltrials.gov) - P2 | N=64 | Recruiting | Sponsor: Beijing InnoCare Pharma Tech Co., Ltd.

Metastases • New P2 trial • Biliary Cancer • Cholangiocarcinoma • Gastrointestinal Cancer • Oncology • Solid Tumor • FGFR2

InnoCare to Present Latest Clinical Data of Gunagratinib at the Upcoming 2023 ASCO GI (Businesswire) - "InnoCare Pharma...announced today that the Company will present the latest clinical data of FGFR inhibitor gunagratinib (ICP-192) for the treatment of cholangiocarcinoma at the 2023 American Society of Clinical Oncology Gastrointestinal (ASCO GI) Cancers Symposium on January 19-21, 2023, which will be held online and offline in San Francisco, U.S."

P2 data • Biliary Tract Cancer • Cholangiocarcinoma • Gastrointestinal Cancer • Oncology

An Efficacy and Safety Study of ICP-192 in Subjects With Bladder Urothelial Cancer (clinicaltrials.gov) - P2 | N=115 | Recruiting | Sponsor: Beijing InnoCare Pharma Tech Co., Ltd. | Trial completion date: Dec 2022 ➔ Jun 2025 | Trial primary completion date: Jun 2022 ➔ Feb 2024

Metastases • Trial completion date • Trial primary completion date • Bladder Cancer • Genito-urinary Cancer • Oncology • Solid Tumor • Urothelial Cancer

Phase I results of gunagratinib (ICP-192), a highly selective irreversible FGFR 1-4 inhibitor in patients with head and neck cancer harboring FGF/FGFR gene aberrations. (ASCO 2022) - P1/2 | "This study demonstrated the anti-tumor activity of gunagratinib in HNC patients carrying FGF/FGFR gene aberrations with an ORR of 33.3%. Gunagratinib is safe and well-tolerated in patients with advanced solid tumors including HNC."

Clinical • P1 data • Anemia • Dyslipidemia • Endocrine Disorders • Head and Neck Cancer • Hematological Disorders • Hypertriglyceridemia • Metabolic Disorders • Nephrology • Oncology • Renal Disease • Solid Tumor • Xerostomia

Latest Data of InnoCare's Robust Oncology Pipelines Presented at the 2022 ASCO Annual Meeting (Businesswire) - "Professor Ye Guo...said, 'This study showed the anti-tumor activity of gunagratinib in HNC patients carrying FGF/FGFR gene aberrations. Gunagratinib is safe and well-tolerated in patients with advanced solid tumors including HNC in this study.'"

Media quote

Latest Data of InnoCare’s Robust Oncology Pipelines Presented at the 2022 ASCO Annual Meeting (Businesswire) - P1/2 | N=56 | NCT03758664 | Sponsor: Beijing InnoCare Pharma Tech Co., Ltd. | "Latest data of InnoCare’s robust oncology pipeline were presented at the 2022 American Society of Clinical Oncology (ASCO) Annual Meeting....12 HNC patients were treated with escalating doses (range: 14mg-22mg) of gunagratinib. Among the 9 HNC patients with FGF/FGFR gene aberrations including FGF amplification and FGFR mutation, who have completed at least one tumor assessment, the overall response rate (ORR) was 33.3%, and the disease control rate (DCR) was 66.7%."

P1 data • Head and Neck Cancer • Oncology • Solid Tumor

[VIRTUAL] Phase I result of ICP-192 (gunagratinib), a highly selective irreversible FGFR inhibitor, in patients with advanced solid tumors harboring FGFR pathway alterations. (ASCO 2021) - P1/2 | "Preclinical data showed that gunagratinib overcomes the acquired resistance to the first-generation reversible FGFR inhibitors, e.g., infigratinib . Gunagratinib is safe and well-tolerated in patients with advanced solid tumors . Anti-tumor activity was demonstrated in patients with FGF/FGFR gene aberrations in multiple tumor types, including cholangiocarcinoma (NCT03758664) . Better response is expected with the increase of treatment durations."

Clinical • P1 data • Biliary Cancer • Cholangiocarcinoma • Dyslipidemia • Gastrointestinal Cancer • Hypertriglyceridemia • Metabolic Disorders • Nephrology • Oncology • Renal Disease • Solid Tumor • FGFR2

InnoCare Presents Latest Clinical Data of pan-FGFR Inhibitor Gunagratinib at the 2021 ASCO Annual Meeting (Yahoo Finance) - "Professor Ye Guo...said, 'Gunagratinib is safe and well-tolerated in patients with advanced solid tumors. Anti-tumor activity was demonstrated in patients with FGF/FGFR geneaberrations in multiple tumor types, including cholangiocarcinoma. Better response is expected with the increase of treatment durations.'"

Media quote

A Clinical Trial of ICP-192 in Treated Patients With Advanced Solid Tumors With FGF/FGFR Gene Alterations (clinicaltrials.gov) - P2 | N=200 | Recruiting | Sponsor: Beijing InnoCare Pharma Tech Co., Ltd.

New P2 trial • Oncology • Solid Tumor

InnoCare Releases 2021 Half Year Results and Business Highlights (PRNewswire) - "ICP-192 (gunagratinib)...Dose escalation in advanced solid tumors, aiming at expanding more indications with higher dose....Phase I trial is expected to complete in the first half of 2022."

Trial completion date • Oncology • Solid Tumor

InnoCare’s pan-FGFR inhibitor picks up ODD in US for cholangiocarcinoma (GBI Health) - "Beijing InnoCare Pharma Tech Co. (09969.HK), a China-based biotech with a focus on cancer and auto-immune diseases, announced having received orphan drug designation (ODD) status from the US FDA for its pan-fibroblast growth factor receptor (FGFR) inhibitor gunagratinib (ICP-192). The targeted indication is cholangiocarcinoma."

Orphan drug • Biliary Tract Cancer • Cholangiocarcinoma • Gastrointestinal Cancer • Oncology

InnoCare Presents Latest Clinical Data of pan-FGFR Inhibitor Gunagratinib at the 2021 ASCO Annual Meeting (Businesswire) - P1/2a, N=56; Sponsor: Beijing InnoCare Pharma Tech Co., Ltd; "As of February 2021, a total of 30 patients had received the treatment of gunagratinib. Gunagratinib performed well in safety and tolerance, the maximum tolerated dose (MTD) had not been reached. Among the 12 patients with FGF/FGFR gene aberrations who have completed at least one tumor assessment, the overall response rate (ORR) was 33.3%, including 1 patient (8.3%) of cholangiocarcinoma with complete response (CR) and 3 patients (25%) with partial response (PR), 7 patients achieved SD. The disease control rate (DCR) was 91.7%."

P1 data • Biliary Tract Cancer • Cholangiocarcinoma • Oncology • Solid Tumor

Clinical Study of ICP-192 in Solid Tumors Patients (clinicaltrials.gov) - P1/2; N=56; Recruiting; Sponsor: Beijing InnoCare Pharma Tech Co., Ltd.; Trial completion date: Jun 2021 ➔ Dec 2024; Trial primary completion date: Dec 2020 ➔ Dec 2024

Clinical • Trial completion date • Trial primary completion date • Oncology • Solid Tumor • FGFR • FGFR2

InnoCare Announces First Subject Dosed in Clinical Trial of ICP-192 in the U.S. (Businesswire) - "InnoCare Pharma...announced today the first subject dosed in clinical trial of pan-FGFR inhibitor ICP-192 in the United States. ICP-192 is a highly selective small-molecule pan-FGFR inhibitor for the treatment of various solid tumors with FGFR aberrations. Currently it is in Phase I/II clinical studies in China and the United States. The Phase II trial in China is a multi-center, open-label clinical trial designed to evaluate the safety and efficacy of ICP-192 in patients with advanced cholangiocarcinoma and urothelial cancer that have FGFR aberrations."

Trial status • Biliary Tract Cancer • Bladder Cancer • Cholangiocarcinoma • Gastrointestinal Cancer • Oncology • Urothelial Cancer

InnoCare Releases 2020 Annual Results and Business Highlights (PRNewswire) - P1/2, N=45; NCT04565275; Sponsor: Beijing InnoCare Pharma Tech Co., Ltd; "ICP-192 (gunagratinib)...Phase I trial of gunagratinib was completed, showing good tolerability. Phase II trials has been progressing well. Of the 30 patients that were dosed, 12 patients with FGF/FGFR gene aberrations, the ORR was 33.3% including 1 cholangiocarcinoma patient (8.3%) achieving CR and 3 patients (25%) with PR. The DCR was 91.7% (11 of 12 patients)"

P1/2 data • Biliary Tract Cancer • Cholangiocarcinoma • Gastric Cancer • Oncology • Solid Tumor • Urothelial Cancer

A Study of ICP-192 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1/2; N=45; Recruiting; Sponsor: Beijing InnoCare Pharma Tech Co., Ltd.

Clinical • New P1/2 trial • Biliary Cancer • Cholangiocarcinoma • Gastrointestinal Cancer • Oncology • Solid Tumor • Urothelial Cancer • FGFR

An Efficacy and Safety Study of ICP-192 in Subjects With Bladder Urothelial Cancer (clinicaltrials.gov) - P2; N=95; Recruiting; Sponsor: Beijing InnoCare Pharma Tech Co., Ltd.

Clinical • New P2 trial • Bladder Cancer • Genito-urinary Cancer • Oncology • Solid Tumor • Urothelial Cancer

Clinical Study of ICP-192 in Solid Tumors Patients (clinicaltrials.gov) - P1/2; N=56; Recruiting; Sponsor: Beijing InnoCare Pharma Tech Co., Ltd.; Phase classification: P1 ➔ P1/2

Clinical • Phase classification