3728 Jinke Rd, Bldg 1, West Wing, Shanghai, China
info@tyligand.com
With support from our investors and trusted collaboration partners, our scientists have built a high-value and risk-balanced pipeline of clinical and pre-clinical stage assets. These molecules serve as multi-targeted therapies for resistant tumors and involve regulating the phosphorylation levels of hydroxyl groups among various types of biomolecules.
The drug modalities under development include small molecules, small molecule conjugates with other small molecules, and large molecules such as antibodies (ADC) and peptides (PDC).
The drug modalities under development include small molecules, small molecule conjugates with other small molecules, and large molecules such as antibodies (ADC) and peptides (PDC).
Tyligand Bioscience Pipeline
Candidates | Target | Indication | Discovery Phase I Phase II | Type |
|---|---|---|---|---|
TSN084 is a globally pioneering multi-kinase inhibitor with proprietary intellectual property rights that targets CDK8/19 and other kinases closely related to tumor proliferation and immune escape. As a type II multi-target kinase inhibitor, it has inhibitory effects on tumors with multiple targets/mechanisms. TSN084 has been approved for clinical trials in China and the United States and a phase I clinical trial for multiple solid tumor types is being conducted in both countries simultaneously. | CDK8/19 | Lung cancer | Multi-kinase | |
TSN222 is a novel bifunctional small molecule designed with sequential and synergistic release of both immune agonism and cytotoxic functions modulated in vivo by pharmacokinetics. It not only activates interferon production in the tumor microenvironment, but also selectively kills tumors cells to prime the adaptive immune system. TSN222’s preclinical data showed good tolerability, excellent tumor suppression efficacy and sustainable immune memory. This product has been granted clinical trial approval in China and the United States and is actively preparing and conducting clinical trials for solid tumors in both countries. | STING | Solid tumors | Tumors | |
KRAS, which stands for Kirsten rat sarcoma viral oncogene homolog, is one of the most commonly mutated oncogenes in human cancer, with G12C being one of the most common mutations of KRAS. Currently, only two KRAS G12C inhibitors have been approved for use globally, namely Sotorasib from Amgen and Krazati from Mirati. TSN333 is an innovative second-generation KRAS G12C inhibitor that has unique differentiating features compared to existing drugs. It has demonstrated excellent efficacy and tolerability against G12C resistance mutations. Compared to currently available inhibitors, TSN333 may have higher potency and lower risk of side effects. The drug has been approved for clinical trials in both China and the United States and is expected to become an important treatment option for KRAS G12C mutations, providing better treatment outcomes and quality of life for patients with KRAS G12C-related cancers. | KRAS | Lung cancer | Nucleoside | |
RAS is the first identified oncogene in human tumors and one of the most widely mutated genes in cancer. Developing targeted drugs to inhibit RAS-driven cancers has long been a challenge, earning it the nickname of an "undruggable" target. The types and probabilities of KRAS mutations vary depending on the tumor tissue type, with most carrying missense mutations, including G12C, G12D, G13V, and others. Among them, KRAS G12D is mainly found in pancreatic cancer, which currently has limited prognoses and treatment options. TSN1611 has unique structural and characteristic advantages, making it superior in toxicity and bioavailability compared to other similar compounds with publicly available information. It has the potential to become one of the best in class pipeline products globally for this target. | KRAS | Pancreatic cancer | Nucleoside Phosphatase Inhibitor |
Collaborations
Candidates | Target | Indication | Discovery Phase I Phase II | Type | Partner |
|---|---|---|---|---|---|
GQ1010 is a potential best-in-class TROP2 ADC that uses Genequantum's unique site-specific conjugation technology, combined with Tyligand’s novel linker payload, to improve the stability, safety and efficacy of ADCs, mainly targeting the treatment of NSCLC, TNBC and other solid tumors. GQ1010 has shown highly differentiated preclinical characteristics: studies have shown that GQ1010 exhibits stronger in vitro cytotoxicity and stronger bystander killing than DS1062 in various Trop2+ cancer cell lines. It exhibits excellent in vivo antitumor activity in different CDX models (including TNBC, gastric cancer, head and neck (H&N) and pancreatic cancer), surpassing DS1062 and Trodelvy® (sacituzumab govitecan-hziy). In vitro plasma stability data confirmed that GQ1010 has a highly stable linker and less effective payload shedding relative to benchmark products. NCI-N87 model showed high target-specific effective payload delivery, with ~90-fold enrichment of effective payload in tumor compared to plasma. In primate toxicology studies, GQ1010 showed excellent tolerability, with no signs of interstitial lung disease (ILD) at a dose of 80mg/kg. Compared with leading TROP2 ADCs, preclinical data suggest that GQ1010 has a potentially wider therapeutic window and stronger efficacy. | TROP2 | Solid | ADC |  | |
PR-positive cancer refers to cancer that expresses excessive progesterone receptors. This type of cancer is commonly seen in breast cancer, ovarian cancer and endometrial cancer. Currently, the FDA-approved treatments for these types of cancers mainly target estrogen receptors, and do not directly intervene in the progesterone signaling pathway. ONA-XR is a novel therapy that selectively inhibits the progesterone signaling pathway to treat PR-positive cancer. It blocks the interaction between progesterone and its receptor, thereby inhibiting the downstream signaling pathways that drive cancer progression. The active ingredient in ONA-XR, Onapristone, is a highly selective progesterone receptor antagonist with a unique chemical structure and biological properties. ONA-XR's clinical trials have shown promising results, demonstrating the ability to inhibit tumor growth in PR-positive breast cancer and endometrial cancer. It may provide a much-needed treatment option for PR-positive cancer patients and improve their survival status.
| PR | Recurrent | Progesterone |  |
