Innovent Presents Phase 1 Clinical Data of IBI351 (KRASG12C Inhibitor) as Monotherapy for Metastatic Colorectal Cancer at the 2023 ASCO Annual Meeting

ROCKVILLE, Md. and SUZHOU, China, June 6, 2023 /PRNewswire/ -- Innovent Biologics, Inc. ("Innovent") (HKEX: 01801), a world-class biopharmaceutical company that develops, manufactures and commercializes high quality medicines for the treatment of oncology, autoimmune, metabolic, ophthalmology and other major diseases, announced the preliminary data of IBI351 (GFH925, KRAS^G12C inhibitor) is presented at the 2023 American Society of Clinical Oncology (ASCO) Annual Meeting.

Efficacy and safety of IBI351 monotherapy in metastatic colorectal cancer harboring KRAS^G12C mutation: preliminary results from a pooled analysis of two Phase 1 studies

Abstract #: 3586

IBI351 is a novel, irreversible covalent inhibitor of KRAS^G12C mutation. Data presented in ASCO 2023 was from a pooled analysis of two Phase 1 studies (NCT05005234, NCT05497336). As of data cutoff date(Feb 16, 2023), a total of 54 metastatic colorectal cancer patients were included for analysis (including 3 subjects at 700mg QD, 4 subjects at 450mg BID, 46 subjects at 600mg BID and 1 subjects at 750mg BID). The study results were as follows:

• Of 42 evaluable subjects at 600mg BID, ORR was 42.9% (18/42), confirmed ORR was 31.0% (13/42), DCR was 88.1% (37/42). A total of 23 subjects at 600mg BID received ≥2 lines of systematic anticancer therapy prior to enrollment. ORR was 65.2% (15/23), confirmed ORR was 43.5% (10/23), DCR was 87.0% (20/23).
• The median duration of response (DoR) was not reached yet, with a median follow-up of 5.5 months. The 3-month DoR rate was 85.7%. As data cutoff, 92.3% of the confirmed responders were remained on treatment.
• As data cutoff, IBI351 was well tolerated. Treatment-related adverse events (TRAEs) occurred in 87.0% (47/54) subjects and the majority of the TRAEs were grade 1-2. The most common TRAEs were anemia, white blood cell count decreased, pruritus, alanine aminotransferase increased, neutrophil count decreased, aspartate aminotransferase increased, blood bilirubin increased and asthenia. About 18.5% subjects reporting grade 3 TRAEs. There were no grade 4-5 TRAEs or TRAEs led to treatment discontinuation.

Favorable safety and tolerability and promising antitumor activity of IBI351 monotherapy were observed in advanced colorectal cancer harboring KRAS^G12C mutation. IBI351 has received NMPA Breakthrough Designation as monotherapy for previous treated advanced non-small cell lung cancer (NSCLC) and colorectal carcinoma in Jan 2023 and May 2023, respectively.

Professor Kefeng Ding from the Second Affiliated Hospital Zhejiang University School of Medicine, stated: "KRAS^G12C mutation occurs in about 2.5% of colorectal cancer in China. The prognosis of advanced colorectal carcinoma patients with KRAS^G12C mutation is worse than KRAS wild type patients with limited therapeutic options. Currently, there are no approved drugs targeting KRAS^G12C available on the market in China. IBI351 is a novel, irreversible covalent inhibitor of KRAS^G12C mutation. The preliminary data shows favorable safety and promising activity of IBI351 monotherapy in KRAS^G12C mutated advanced colorectal cancer. We look forward to more positive clinical data from this study. "

Dr. Hui Zhou, Senior Vice President of Innovent, stated: "We are pleased to present our clinical development results of IBI351 in advanced colorectal cancer at the 2023 ASCO. As a highly effective oral inhibitor of KRAS^G12C, IBI351 has shown encouraging efficacy and safety signals in a variety of advanced solid tumors and has received Breakthrough Designation by CDE for NSCLC and colorectal cancer. The data reported at ASCO 2023 showed that IBI351 monotherapy has excellent efficacy and safety in previously treated advanced colorectal carcinoma. We look forward to obtaining more data from the ongoing clinical trials, and further explore the efficacy and safety of IBI351 as monotherapy or combination therapy in patients with advanced colorectal carcinoma. "

About Colorectal Carcinoma (CRC)

According to GLOBOCAN 2020 report, there were about 1.93 million new cases of colorectal cancer worldwide in 2020, and caused about 930,000 deaths[1]. In the past 30 years, the number of CRC cases and deaths has continued to increase. In 2015, there were 376,000 new cases and 191,000 deaths, and the new CRC cases and deaths will continue to increase in the next 25 years, which is a major public health problem in China. KRAS^G12C is a specific KRAS mutation subtype that causes KRAS to be in a state of sustained GTP-binding activation. KRAS^G12C mutation is present in about 3% of colorectal cancer patients in the Western population and 2.5% of Chinese colorectal cancer patients[2].

About IBI351 (GFH925,KRAS^G12C Inhibitor)

Discovered by GenFleet Therapeutics, GFH925 (Innovent R&D code: IBI351) is a novel, orally active, potent KRAS^G12C inhibitor designed to effectively target the GTP/GDP exchange, an essential step in pathway activation, by modifying the cysteine residue of KRAS^G12C protein covalently and irreversibly. Preclinical cysteine selectivity studies demonstrated high selectivity of IBI351 towards G12C. Subsequently, IBI351 effectively inhibits the downstream signal pathway to induce tumor cells' apoptosis and cell cycle arrest.

In September 2021, Innovent and GenFleet Therapeutics entered into an exclusive license agreement for the development and commercialization of IBI351 in China (including mainland China, Hong Kong, Macau and Taiwan) with additional option-in rights for global development and commercialization.

About Innovent

Inspired by the spirit of "Start with Integrity, Succeed through Action," Innovent's mission is to develop, manufacture and commercialize high-quality biopharmaceutical products that are affordable to ordinary people. Established in 2011, Innovent is committed to developing, manufacturing and commercializing high-quality innovative medicines for the treatment of cancer, autoimmune disease, metabolic disorder and other major diseases. On October 31, 2018, Innovent was listed on the Main Board of the Stock Exchange of Hong Kong Limited with the stock code: 01801.HK.

Since its inception, Innovent has developed a fully integrated multi-functional platform which includes R&D, CMC (Chemistry, Manufacturing, and Controls), clinical development and commercialization capabilities. Leveraging the platform, the company has built a robust pipeline of 35 valuable assets in the fields of cancer, metabolic disorder, autoimmune disease and other major therapeutic areas, with 8 approved products on the market. These include: TYVYT® (sintilimab injection), BYVASDA®(bevacizumab biosimilar injection), SULINNO® (adalimumab biosimilar injection), HALPRYZA®(rituximab biosimilar injection), Pemazyre®(pemigatinib oral inhibitor), olverembatinib (BCR ABL TKI), Cyramza® (ramucirumab) and Retsevmo®(selpercatinib). An additional 3 assets are under NMPA NDA review, 6 assets are in Phase 3 or pivotal clinical trials, and 18 more molecules are in clinical studies.

Innovent has built an international team with advanced talent in high-end biological drug development and commercialization, including many global experts. The company has also entered into strategic collaborations with Eli Lilly and Company, Sanofi, Adimab, Incyte, MD Anderson Cancer Center and other international partners. Innovent strives to work with many collaborators to help advance China's biopharmaceutical industry, improve drug availability and enhance the quality of the patients' lives. For more information, please visit: www.innoventbio.com. and www.linkedin.com/company/innovent-biologics/. 

Disclaimer: Innovent does not recommend any off-label usage.

Note:
TYVYT® (sintilimab injection) is not an approved product in the United States.

BYVASDA® (bevacizumab biosimilar injection), SULINNO®, and HALPRYZA® (rituximab biosimilar injection) are not approved products in the United States.
TYVYT® (sintilimab injection, Innovent)
BYVASDA® (bevacizumab biosimilar injection, Innovent)
HALPRYZA® (rituximab biosimilar injection, Innovent)
SULINNO® (adalimumab biosimilar injection, Innovent)
Pemazyre® (pemigatinib oral inhibitor, Incyte Corporation). Pemazyre® was discovered by Incyte Corporation and licensed to Innovent for development and commercialization in Mainland China, Hong Kong, Macau and Taiwan.
CYRAMZA® (ramucirumab, Eli Lilly). CYRAMZA® was discovered by Eli Lilly and licensed to Innovent for commercialization in Mainland China.
Retsevmo®(selpercatinib, Eli Lilly). Retsevmo® was discovered by Eli Lilly and licensed to Innovent for commercialization in Mainland China.

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