Qilu Pharmaceutical's PROTAC Drug QLH12016 Granted IND Approval for Advanced Prostate Cancer and Other Solid Tumors

On August 22, Qilu Pharmaceutical Group's WeChat Official Account published an article stating that according to the implied permission column for clinical trials on the official website of the Center for Drug Evaluation (CDE) of the National Medical Products Administration, Qilu Pharmaceutical's Class 1 new drug QLH12016 capsule has been approved for clinical use and can be used to treat malignant solid tumors, including advanced prostate cancer.

QLH12016 capsule is a PROTAC (Proteolysis Targeting Chimera) product developed by Qilu Pharmaceutical. PROTAC technology represents a cutting-edge direction in small-molecule targeted drugs, with exploratory applications in oncology and various non-oncological diseases. By employing novel molecular design techniques, it achieves targeted protein degradation, enabling the targeting of undruggable targets by traditional methods or addressing resistance to existing targeted drugs. Additionally, it exhibits event-driven characteristics, offering advantages over traditional small-molecule drugs such as longer duration of action, higher potency, or lower effective dosage.

The incidence of prostate cancer has risen to the third most common malignant tumor globally. Although there are currently available treatments for metastatic castration-resistant prostate cancer (mCRPC), patients who do not respond well to or cannot be adequately controlled by existing therapies still face the risk of disease progression and high rates of distant bone metastases, significantly impacting their survival time and quality of life. Therefore, there remains an urgent clinical need for more effective treatment strategies to further improve survival benefits for such patients.

PROTAC technology drugs are protein degraders developed based on the ubiquitin-proteasome system. Their structure includes a target protein ligand, a linker, and an E3 ligase ligand. The target protein ligand can specifically bind to the target protein, while the other end recruits E3 ligase to form a ternary complex. E3 ligase can mediate the ubiquitination of the target protein by E3 ubiquitin-conjugating enzyme. The ubiquitin-tagged target protein is recognized and degraded by the proteasome.

Qilu Pharmaceutical, in the development and research of QLH12016, has focused on unmet clinical needs by conducting comparative studies with similar products. It implemented differentiated design during the early molecular construction phase and systematically designed in vivo and in vitro experiments based on the PROTAC molecule, target characteristics, and core development objectives during the non-clinical research process. QLH12016 demonstrated significant features of a novel molecular mechanism and superior tumor suppression effects both in vivo and in vitro, showing favorable drug-like properties. QLH12016 is expected to provide patients with a new treatment option.

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