Our in-house discovery engine has created a broad pipeline of more than ten clinical stage investigational drug candidates with several more in preclinical testing. These drug candidates cover both novel and validated targets, including MET, VEGFR, FGFR, CSF-1R, PI3Kδ, Syk, IDH, ERK, EGFR, BTK and CD47, amongst others, and some are being investigated both as potential single agents and in combinations. Our success in discovery has also led to development collaborations with leading global pharmaceutical companies such as AstraZeneca and Eli Lilly.
For investors, more information can be found under the Shareholder Information section of this website.
The safety and efficacy of the agents and/or uses under investigation have not been established. There is no guarantee that the agents will receive health authority approval or become commercially available in any country for the uses being investigated.
Updated as of May 11, 2022.
* Phase II registration-intent study subject to regulatory discussion; ** In planning; *** Investigator-initiated trials (IIT)；**** Development in collaboration with Epizyme.
Notes: MAA = Marketing Authorization Application; MET = mesenchymal epithelial transitior; NSCLC = non-small cell lung cancer; EGFRm = epidermal growth factor receptor mutation; RCC = renal cell carcinoma; VEGFR = vascular endothelial growth factor receptor; TKI = tyrosine kinase inhibitor; FGFR 1 = fibroblast growth factor receptor 1; CSF-1R = colony stimulating factor-1 receptor; NET = neuroendocrine tumors; NEC = neuroendocrine carcinoma; ESCC = esophageal cancer; GC = gastric cancer; SCLC = small cell lung cancer; BTC = biliary tract cancer; TC = thyroid cancer; EMC = endometrial cancer; TN = triple negative; CRC = colorectal cancer; HCC = hepatocellular carcinoma; GI = gastrointestinal; PI3Kδ = Phosphatidylinositol-3-Kinase delta; NHL = Non-Hodgkin’s Lymphoma; PTCL = peripheral T-cell lymphoma; FL = follicular lymphoma; MZL = marginal zone lymphoma; MCL = mantle cell lymphoma; DLBCL = diffuse large B cell lymphoma; CLL/SLL = chronic lymphocytic leukemia/small lymphocytic lymphoma; HL = Hodgkin’s lymphoma; Syk = spleen tyrosine kinase; ITP = immune thrombocytopenic purpura; wAIHA = warm autoimmune hemolytic anemia; EZH2 = enhancer of zeste homolog 2; IHCC = intrahepatic cholangiocarcinoma; IDH 1/2 = isocitrate dehydrogenase 1/2; ERK = extracellular-signal-regulated kinase; MAPK pathway = RAS-RAF-MEK-ERK signaling cascade; BTK = Bruton's tyrosine kinase; TGCT = Tenosynovial Giant Cell Tumors.
Savolitinib is an investigational inhibitor of the mesenchymal epithelial transition factor, or MET, receptor tyrosine kinase, an enzyme which has been shown to function abnormally in many types of solid tumors. We designed savolitinib through chemical structure modification to specifically address kidney toxicity, the primary issue that halted development of several other selective MET inhibitors.
We are currently investigating savolitinib in global partnership with AstraZeneca, both as a monotherapy and in combination with immunotherapy and targeted therapy.
Savolitinib has been approved and marketed in China under the brand name ORPATHYS®. Savolitinib is not approved for use outside of China.
Surufatinib is a novel, oral angio-immuno kinase inhibitor that inhibits the tyrosine kinase activity associated with vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR), which both inhibit angiogenesis, and colony stimulating factor-1 receptor (CSF-1R), which regulates tumor-associated macrophages.
Surufatinib has been approved and marketed in China under the brand name SULANDA®. Surufatinib is not approved for use outside of China.
In mid-2021 we submitted a Marketing Authorisation Application in Europe for surufatinib for the treatment of pancreatic and non-pancreatic neuroendocrine tumors.
We own all rights to surufatinib globally.
Fruquintinib is a selective and potent oral inhibitor of three vascular endothelial growth factor receptors, known as VEGFR 1, 2 and 3. VEGFR is a receptor tyrosine kinase which contributes to angiogenesis, the buildup of new blood vessels around a tumor, thereby contributing to the growth of tumors.
We are currently studying fruquintinib in colorectal cancer, gastric cancer and various other solid tumors. Studies with fruquintinib are being conducted both as monotherapy and as combination therapy with immunotherapy, targeted therapy and chemotherapy drugs.
Fruquintinib has been approved and marketed in China under the brand name ELUNATE®. In the United States, it was granted Fast Track Designation by the FDA. Fruquintinib is not approved for use outside of China.
The investigational drug candidate amdizalisib is a novel, selective small molecule inhibitor targeting the isoform phosphoinositide 3’-kinase delta (PI3Kδ), a key component in the B-cell receptor signaling pathway. We have designed amdizalisib with increased PI3Kδ isoform selectivity. Amdizalisib ’s pharmacokinetic properties have been found to be favorable with good oral absorption, moderate tissue distribution and low clearance in pre-clinical pharmacokinetic studies.
Amdizalisib is being investigated in studies in the U.S., Europe, China and Australia in various subtypes of advanced relapsed or refractory non-Hodgkin's lymphoma, including follicular lymphoma and marginal zone lymphoma.
We currently retain all rights to amdizalisib worldwide.
The investigational drug candidate HMPL-523 is a novel, selective, oral inhibitor of the spleen tyrosine kinase (Syk).
Syk is a major component in B-cell receptor signaling and is an established therapeutic target in multiple subtypes of B-cell lymphomas. Because B-cell malignancies are heterogeneous and patients commonly experience relapse despite current therapies, there is a need for new therapies. Syk is upstream of both BTK and PI3K.
HMPL-523 is being investigated in various hematological cancers such as indolent non-Hodgkin's lymphomas and certain chronic immune diseases in the U.S., Europe, China and Australia.
We currently retain all rights to HMPL-523 worldwide.
Tazemetostat is a methyltransferase inhibitor of EZH2 developed by Epizyme, Inc. EZH2 catalyzes the methylation of histone H3 which controls expression of various genes and in turn plays a role in the normal physiology of many cell types. Dysregulation of EZH2 has been seen in a wide range of cancers and is associated with poor clinical prognosis and outcomes.
We have a strategic collaboration with Epizyme to research, develop, manufacture and commercialize tazemetostat in Greater China. We are exploring the treatment potential of tazemetostat in investigational clinical trials in other solid tumors and hematological malignancies, as a monotherapy and combination therapy in both relapsed and front-line disease settings.
Tazemetostat is approved in the US under the brand name TAZVERIK®. Tazemetostat is not approved for use outside of the U.S.
HMPL-453 is an investigational novel selective small molecule inhibitor that targets fibroblast growth factor receptor (FGFR) 1/2/3, a sub-family of receptor tyrosine kinases. Aberrant FGFR signaling has been found to be a driving force in tumor growth (through tissue growth and repair), promotion of angiogenesis and resistance to anti-tumor therapies. Abnormal FGFR gene alterations are believed to be the drivers of tumor cell proliferation in several solid tumor settings.
We currently retain all rights to HMPL-453 worldwide.
HMPL-306 is an investigational novel selective small molecule dual inhibitor of isocitrate dehydrogenase (IDH) 1 and 2 mutations. IDH1 and IDH2 mutations have been implicated as drivers of certain hematological malignancies, gliomas and solid tumors, particularly among acute myeloid leukemia patients. Cytoplasmic mutant IDH1 and mitochondrial mutant IDH2 have been known to switch to the other form when targeted by an inhibitor of IDH1 mutant alone or IDH2 mutant alone. Cancer patients harboring either IDH mutation have been known to develop resistance to therapies that target IDH1 or IDH2 through isoform switching.
We currently retain all rights to HMPL-306 worldwide.
HMPL-295 is a novel investigational inhibitor of ERK. ERK is a downstream component of the RAS-RAF-MEK-ERK signaling cascade (MAPK pathway). This is our first of multiple candidates in discovery targeting the MAPK pathway.
RAS-MAPK pathway is dysregulated in human diseases, particularly cancer, in which mutations or non-genetic events hyper-activate the pathway in more than 50% of cancers. Activating mutations in RAS genes occur in more than 30% of cancers. RAS and RAF predict worse clinical prognosis in a wide variety of tumor types, mediate resistance to targeted therapies, and decrease the response to the approved standards of care. In the MAPK pathway, KRAS inhibitors are under clinical evaluation, and acquired resistance develops for RAF/MEK targeted therapies. ERK inhibition has the potential to overcome or avoid the intrinsic or acquired resistance from upstream mechanisms such as these.
We currently retain all rights to HMPL-295 worldwide.
HMPL-760 is a novel third-generation BTK inhibitor and our eleventh in-house discovered small molecule investigational oncology drug candidate. It is a reversible, non-covalent inhibitor of BTK wild type and BTK C481S mutant enzymes. C481S is a key resistance mechanism for first-generation BTK inhibitors.
We currently retain all rights to HMPL-760 worldwide.
A significant portion of patients with non-small cell lung cancer go on to develop brain metastasis. Patients with brain metastasis suffer from poor prognosis. Epitinib is a selective oral epidermal growth factor receptor (EGFR) inhibitor. Investigational studies suggest that epitinib may overcome the blood-brain barrier.
We currently retain all rights to epitinib worldwide.
Like epitinib, theliatinib is an investigational novel molecule epidermal growth factor receptor (EGFR) inhibitor under investigation for the treatment of solid tumors. Theliatinib has been designed with strong affinity to the wild-type EGFR kinase. Theliatinib has been investigated in patients with esophageal and head & neck cancer, tumor-types with a high incidence of wildtype EGFR activation.
We currently retain all rights to theliatinib worldwide.