Biopharmaceutical Company Announces First Patient Dosed In Cancer Treatment Trial
Biopharmaceutical Company Announces First Patient Dosed In Cancer Treatment Trial
Verastem Oncology Announces First Patient Dosed in Phase 1/2 Trial of GFH375/VS-7375 in China.
Disclaimer: The following article is for informational purposes only and should not be considered as medical advice. All information provided is based on recent announcements and data pertaining to the development of GFH375/VS-7375 by Verastem Oncology and GenFleet Therapeutics. Readers should consult with healthcare professionals for medical advice and treatment options.
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Verastem Oncology, a biopharmaceutical company listed on Nasdaq under the ticker VSTM, has recently announced the commencement of dosing for the first patient in a Phase 1/2 clinical trial in China. This trial, conducted by GenFleet Therapeutics, aims to evaluate GFH375/VS-7375, a novel KRAS G12D (ON/OFF) inhibitor.
The Development of GFH375/VS-7375
GFH375/VS-7375 was identified as Verastem’s lead discovery program from its collaboration with GenFleet Therapeutics, established in 2023. The compound is an oral, potent, and selective KRAS G12D dual inhibitor targeting both the active (GTP) and inactive (GDP) states of the KRAS protein. Preclinical data presented at the American Association for Cancer Research (AACR) Annual Meeting in April 2024 demonstrated its promising potential. The data showed oral bioavailability across multiple preclinical species, strong anti-tumor activity as a single agent, and potency against intracranial tumor models, suggesting it could effectively treat brain metastases.
Dan Paterson, President and CEO of Verastem Oncology, highlighted the rapid progress made in developing GFH375/VS-7375. "In a short amount of time, we identified GFH375/VS-7375, a novel KRAS G12D (ON/OFF) inhibitor, as our lead discovery program last year and now the first patient has been dosed in the Phase 1/2 study by GenFleet in China," said Paterson. He expressed optimism about leveraging initial clinical dose escalation data to accelerate development in the U.S., particularly given the lack of FDA-approved KRAS G12D-targeted treatments despite the mutation's high prevalence in various cancers, including pancreatic, colorectal, lung, and uterine cancers.
The Phase 1 study is being conducted in approximately 20 hospitals across China. Its primary objective is to evaluate the safety and efficacy of GFH375/VS-7375 in patients with advanced KRAS G12D mutant solid tumors. This part of the study will determine the recommended Phase 2 dose (RP2D). Subsequently, Phase 2 will further assess the efficacy and safety of GFH375/VS-7375 in patients with advanced solid tumors, such as pancreatic ductal adenocarcinoma, colorectal cancer, and non-small cell lung cancer.
Importance of KRAS G12D Inhibition
The KRAS gene plays a critical role in cellular signal transduction. Mutations in KRAS, such as the G12D variant, are frequently implicated in the development and progression of various cancers. These mutations lead to continuous activation of the KRAS protein, promoting uncontrolled cell division and tumorigenesis. Despite its importance, targeting KRAS has been historically challenging due to its structure and the nature of its interactions within the cell. GFH375/VS-7375 represents a novel approach by inhibiting both the ON (GTP-bound) and OFF (GDP-bound) states of KRAS G12D. This dual inhibition strategy aims to disrupt the oncogenic signaling pathways driven by KRAS mutations, potentially offering a new and effective treatment option for patients with KRAS G12D-mutant cancers.
The preclinical development of GFH375/VS-7375 has shown promising results, which were presented at the AACR Annual Meeting in April 2024. The compound demonstrated excellent oral bioavailability across various preclinical species, indicating its potential for effective oral administration in humans. The preclinical studies revealed strong anti-tumor activity when used as a single agent, revealing its potential efficacy in treating cancers harboring KRAS G12D mutations. One of the most compelling aspects of the preclinical data was GFH375/VS-7375's potency against intracranial tumor models. This suggests that the compound could cross the blood-brain barrier and target brain metastases, a common and challenging complication in advanced cancer patients. If these preclinical findings translate into clinical success, GFH375/VS-7375 could address a unmet need in oncology.
Collaboration Between Verastem Oncology and GenFleet Therapeutics
The collaboration between Verastem Oncology and GenFleet Therapeutics has been instrumental in advancing the development of GFH375/VS-7375. Established in 2023, this partnership focuses on three discovery programs, with the KRAS G12D inhibitor being the first and leading project. GenFleet’s Investigational New Drug (IND) application for GFH375/VS-7375 was approved in China in June 2024, paving the way for the initiation of the Phase 1/2 trial and the dosing of the first patient in July 2024.
The collaboration agreement includes provisions for Verastem Oncology to obtain exclusive options to license the three compounds selected for the partnership after achieving pre-determined milestones in Phase 1 trials. These licenses would grant Verastem Oncology development and commercialization rights outside GenFleet’s territories, which include mainland China, Hong Kong, Macau, and Taiwan. Verastem Oncology is a late-stage development biopharmaceutical company dedicated to developing and commercializing new medicines to improve the lives of cancer patients. The company’s pipeline primarily focuses on RAS/MAPK-driven cancers, targeting critical signaling pathways that promote cancer cell survival and tumor growth. Verastem’s approach includes the development of novel small molecule drugs that inhibit key pathways, such as RAF/MEK and FAK inhibition.
GenFleet Therapeutics, based in China, specializes in innovative therapeutics for oncology and immunology. The company’s focus on precision medicine and its robust research capabilities have facilitated the rapid advancement of several promising drug candidates, including GFH375/VS-7375. The initiation of the Phase 1/2 trial for GFH375/VS-7375 marks a milestone in the collaborative efforts of Verastem Oncology and GenFleet Therapeutics. With the dosing of the first patient in China, the trial aims to evaluate the safety and efficacy of this novel KRAS G12D (ON/OFF) inhibitor in patients with advanced solid tumors. The promising preclinical data coupled with the collaboration between Verastem and GenFleet offers hope for the development of an effective treatment for cancers driven by KRAS G12D mutations.
As the clinical trial progresses, the oncology community will closely monitor the outcomes, particularly regarding safety, efficacy, and the potential to address unmet needs in cancer treatment. Should GFH375/VS-7375 demonstrate positive results, it could pave the way for new therapeutic options for patients with KRAS G12D-mutant cancers, ultimately improving their prognosis and quality of life.
Disclaimer: The content provided in this article is for informational purposes only and does not constitute medical advice. Readers are encouraged to seek professional medical guidance for their specific health concerns and treatment options.
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