Home / Pipeline

Keythera Biopharmaceuticals, as a clinical-stage innovative pharmaceutical company rooted in China with a global vision, has achieved breakthrough progress in areas of unmet clinical needs such as oncology and autoimmune diseases. This is accomplished through its proprietary Affinity-based Mass Spectrometry Screening platform. The company has established multiple differentiated pipelines with global competitiveness, three of which have advanced to clinical development stages, demonstrating its highly efficient R&D capabilities.

Project
Indication
Drug Discovery
Clinical candidate compounds
IND
Phase Ia Clinical
Phase Ib Clinical
Phase Ⅱ Clinical

KF-0210

CRC,LC,GC,BC,SCCE

Osteoarthritis (OA)

KBP-2205

Solid Tumor

KBP-2506

Allergies, dermatitis

Two undisclosed

Oncology, Autoimmune

KF-0210: It is a highly selective and potent EP4 receptor antagonist. By modulating the tumor microenvironment and inflammatory responses, it plays a key role in tumor immune escape, inflammatory signaling, and articular cartilage metabolism.

R&D Progress

01Oncology

Completed a Phase 1a dose-escalation study in China and Australia,respectively.Initiated a multi-center Phase 1b trial in combination with the anti-PD-L1 antibody atezolizumab for advanced solid tumors (including non-small cell lung cancer, gastric cancer, and colorectal cancer etc.,). The aim of clinical trial design to evaluate the synergistic effect, particularly the reversal effect in patients who were resistant to immunotherapy.
02Osteoarthritis (OA)

The drug has been approved by NMPA to initiate Phase 2 clinical trials for osteoarthritis, becoming the first EP4 antagonist in China for a disease-modifying therapy of OA. Pre-clinical results demonstrated its multiple effects, including analgesic, anti-inflammatory, and cartilage regenerative properties, highlighting its significant potential as a disease-modifying therapeutic approach for osteoarthritis.

KBP-2506

KBP-2506 is a highly selective small-molecule MRGPRX2 antagonist that demonstrates breakthrough therapeutic potential for immune-inflammatory diseases such as Chronic Urticaria (CU) and Atopic Dermatitis (AD), which are caused by abnormal activation of mast cells. As a novel targeted therapeutic agent, KBP-2506 can effectively inhibits calcium influx and degranulation of LAD2 mast cells by specifically blocking the MRGPRX2 receptor signaling pathway on the surface of mast cells . significantly reduce the release of key inflammatory mediators ,such as histamine, trypsin, and cytokines,and thereby , regulate the abnormal immune response from the source of the disease.

In MRGPRX2 humanized genetically modified animal models, KBP-2506 demonstrated excellent in vivo activity. With outstanding oral bioavailability, favorable pharmacokinetic profile, and a broad therapeutic window, it holds promise as a best-in-class therapy in the field of dermatology.

KBP-2205

KBP-2205 is a highly selective second-generation poly(ADP-ribose) polymerase 1 (PARP1) inhibitor, developed based on innovative molecular design, featuring precise targeting and excellent drugability properties. Preclinical study results demonstrated that KBP-2205 effectively mitigates the risk of hematological toxicity caused by inhibition of PARP2 , exhibiting a superior therapeutic window. In various homologous recombination repair (HRD)-deficient tumor models, KBP-2205 demonstrates potent antitumor activity. Its high oral bioavailability and favorable pharmacokinetic profile support a once-daily dosing regimen.

KBP-2205 has currently initiated Phase 1/2 clinical studies, designed to evaluate its safety, pharmacokinetic profile, and preliminary efficacy in patients with advanced solid tumors. Given its precise targeting mechanism, superior DNA-trapping activity, and optimized therapeutic window, this agent holds promise for providing a safer and more durable targeted therapeutic option for cancer patients with BRCA mutations or other HRD characteristics . especially having significant clinical value for those who are resistant to traditional PARP inhibitors or sensitive to hematological toxicity .