PIPELINE

Orelabrutinib is a highly selective BTK inhibitor developed by InnoCare. As a novel BTK inhibitor, orelabrutinib has high selectivity due to its innovative compound structure, which results in exceptional target occupancy and good efficacy and safety profile. In 2020, orelabrutinib was approved for the treatment of patients with relapsed/refractory (r/r) chronic lymphocytic leukemia (CLL) /small lymphocytic lymphoma (SLL) in China. In 2021, orelabrutinib was included into National Reimbursement Drug list to better benefit lymphoma patients.

According to the latest data, the overall response rate (ORR) was 93.8%, with complete response (CR) of 30%.

More data can be found in the article published at American Journal Of Hematology.

CLL/SLL, one of the most common types of leukemia, is an indolent malignancy of B lymphocytes. Although CLL/SLL is indolent, some patients will progress over time. There are 191,000 newly diagnosed CLL cases and 61,000 deaths every year globally.

Orelabrutinib was included in the CSCO Guidelines and has been recommended as a Class I treatment for r/r CLL/SLL. It has also won multiple innovation awards.

Orelabrutinib is a highly selective BTK inhibitor developed by InnoCare. As a novel BTK inhibitor, orelabrutinib has high selectivity due to its innovative compound structure, which results in exceptional target occupancy and good efficacy and safety profile. Orelabrutinib was approved for the treatment of patients with r/r mantle cell lymphoma (MCL) in China in 2020, included into National Reimbursement Drug list to benefit more lymphoma patients in 2021, and approved for marketing in Singapore in 2022.

According to the latest data, the ORR was 83% with CR of 36.8%.

More data can be found in the article published at Blood Advances, part of leading hematology journal Blood.

MCL is a subtype of B-cell non-Hodgkin lymphoma that results from malignant transformation of B-lymphocytes in the mantle zone of lymph node follicles. Despite high response rates after first-line hemo-immunotherapy, the majority of patients relapse and require subsequent treatment. There is no standard therapy for relapsed/refractory MCL, and the therapies approved by the U.S. Food and Drug Administration for this patient population are still limited, with low rates of CR, short durations of remission, and unfavorable safety and tolerability for older patients.

Orelabrutinib was included in the CSCO Guidelines and has been recommended as a Class I treatment for r/r CLL/SLL. It has also won multiple innovation awards.

Orelabrutinib is a highly selective BTK inhibitor developed by InnoCare. As a novel BTK inhibitor, orelabrutinib has high selectivity due to its innovative compound structure, which results in exceptional target occupancy and good efficacy and safety profile.

MCL is a subtype of B-cell non-Hodgkin lymphoma (NHL) that results from malignant transformation of B-lymphocytes in the mantle zone of lymph node follicles. There is no standard therapy for r/r MCL, and the therapies approved by the FDA for this patient population are still limited, with low rates of CR, short durations of remission, and unfavorable safety and tolerability for older patients. Orelabrutinib was granted as Breakthrough Therapy Designation for the treatment of r/r MCL by U.S. FDA.

Orelabrutinib is a highly selective BTK inhibitor developed by InnoCare. As a novel BTK inhibitor, orelabrutinib has high selectivity due to its innovative compound structure, which results in exceptional target occupancy and good efficacy and safety profile.

Orelabrutinib is a highly selective BTK inhibitor developed by InnoCare. As a novel BTK inhibitor, orelabrutinib has high selectivity due to its innovative compound structure, which results in exceptional target occupancy and good efficacy and safety profile. Orelabrutinib was approved for the treatment of patients with r/r marginal zone lymphoma (MZL) in China in April 2023, and included in the updated National Reimbursement Drug List (NRDL) 2023, thus becoming the first and only approved BTK inhibitor in mainland China. The Company is initiating a Phase III MZL confirmatory study with orelabrutinib.

According to latest data, the ORR assessed by an Independent Review Committee (IRC) was 58.9%, and tumor reduction was observed in 92.2% of patients.

More data can be found in the article published at American Journal Of Hematology.

Orelabrutinib was included in the CSCO Guidelines and has been recommended as a Class I treatment for second-line therapy of MZL.

Orelabrutinib is a highly selective BTK inhibitor developed by InnoCare. As a novel BTK inhibitor, orelabrutinib has high selectivity due to its innovative compound structure, which results in exceptional target occupancy and good efficacy and safety profile.

Orelabrutinib is a highly selective BTK inhibitor developed by InnoCare. As a novel BTK inhibitor, orelabrutinib has high selectivity due to its innovative compound structure, which results in exceptional target occupancy and good efficacy and safety profile.

CLL/SLL, one of the most common types of leukemia, is an indolent malignancy of B lymphocytes. There are 191,000 newly diagnosed CLL cases and 61,000 deaths every year globally.

Orelabrutinib is a highly selective BTK inhibitor developed by InnoCare. As a novel BTK inhibitor, orelabrutinib has high selectivity due to its innovative compound structure, which results in exceptional target occupancy and good efficacy and safety profile. The Company is initiating a global Phase III trial of orelabrutinib for the first-line treatment of MCL.

MCL is a subtype of B-cell non-Hodgkin lymphoma that results from malignant transformation of B-lymphocytes in the mantle zone of lymph node follicles. MCL occurs most frequently in men at a median age of 60 years, and the majority of patients are in an advanced stage of disease when diagnosed.

Tafasitamab is a humanized Fc-modified CD19 targeting immunotherapy, mediating B-cell lysis through apoptosis and immune effector mechanism. Tafasitamab in combination with lenalidomide has been approved for the treatment of relapsed/refractory diffuse large B-cell lymphoma (r/r DLBCL) in China. It is the first CD19 monoclonal antibody approved in China for patients with r/r DLBCL.

The tafasitamab combination regimen received a Grade I Recommendation for second‑line and subsequent‑line treatment of diffuse large B‑cell lymphoma (DLBCL) in the 2026 CSCO Lymphoma Diagnosis and Treatment Guidelines. Results from the global Phase III frontMIND study of the tafasitamab regimen were published in The Lancet, a top‑tier international medical journal, and featured as a high‑impact oral presentation at the plenary session of the 2026 European Hematology Association (EHA) Annual Congress. The results demonstrated that, compared with R‑CHOP, the current first‑line standard‑of‑care, the tafasitamab regimen significantly prolonged progression‑free survival (PFS), with the potential to establish a new first‑line standard‑of‑care for patients with DLBCL.

Final five-year results showed that tafasitamab plus lenalidomide followed by tafasitamab monotherapy provided prolonged, durable responses in adult patients with r/r DLBCL. The ORR was 57.5% (primary endpoint).

DLBCL is the most common type of NHL, accounting for 31%~34% of NHL patients globally. In China, DLBCL accounts for 45.8% of all NHLs.

Mesutoclax is a novel, orally bioavailable BCL2 selective inhibitor. BCL2 is an important regulatory protein in the apoptosis pathway, and its abnormal expression is associated with the development of various hematologic malignancies. Mesutoclax exerts anti-tumor activity by selectively inhibiting BCL2 and restoring the normal apoptosis process in cancer cells. Mesutoclax has been granted two Breakthrough Therapy Designations (BTD) by the CDE.

The head-to-head registrational Phase III trial of mesutoclax with azacitidine versus venetoclax with azacitidine in treatment naïve (TN) acute myeloid leukemia (AML) was initiated in China, with overall survival (OS) as the primary endpoint.

Mesutoclax (ICP-248) is a novel, orally bioavailable BCL2 selective inhibitor developed by InnoCare. BCL2 is an important part of apoptotic pathway and is overexpressed in a variety of hematologic malignancies. Mesutoclax has an anti-tumor effect by selectively inhibiting BCL2 and restoring the mechanism of programmed cell death. Mesutoclax is the first BCL2 inhibitor to receive BTD recognition in China for the treatment of BTKi-treated mantle cell lymphoma. The Phase III registrational trial of mesutoclax in combination with orelabrutinib for the first-line treatment of chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) is advancing.

Mesutoclax in combination with orelabrutinib will achieve deeper remissions in treatment-naive patients with CLL/SLL, prevent the development of resistant mutations, and provide hope for clinical cure, making it a therapeutic regimen with great potential. Data presented at the 2026 ASCO Annual Meeting showed that the combination achieved an overall response rate (ORR) of 100% in 1L CLL/SLL.

Mesutoclax (ICP-248) is a novel, orally bioavailable BCL2 selective inhibitor developed by InnoCare. BCL2 is an important part of apoptotic pathway and is overexpressed in a variety of hematologic malignancies. Mesutoclax has an anti-tumor effect by selectively inhibiting BCL2 and restoring the mechanism of programmed cell death. Mesutoclax is the first BCL2 inhibitor to receive BTD recognition in China for the treatment of BTKi-treated mantle cell lymphoma. Data presented at the 2025 ASH Annual Meeting demonstrated an ORR of 84.0% among MCL patients who were BTK inhibitor refractory.

The registrational Phase III clinical trial of mesutoclax in combination with orelabrutinib in r/r MCL is ongoing in China. Phase I data presented at the 2026 ASCO Annual Meeting demonstrated that the combination regimen achieved an ORR of 100% in patients with r/r MCL.

Mesutoclax (ICP-248), in combination with orelabrutinib, has been granted Breakthrough Therapy Designation (BTD) by the Center for Drug Evaluation (CDE) of the China National Medical Products Administration (NMPA) for the treatment of patients with marginal zone lymphoma (MZL) who have received at least one prior therapy.

Data presented at the 2026 ASCO Annual Meeting demonstrated that the combination achieved an ORR of 100%, with an excellent efficacy and safety, in this patient population.

Mesutoclax (ICP-248) is a novel, orally bioavailable BCL2 selective inhibitor developed by InnoCare. BCL2 is an important part of apoptotic pathway and is overexpressed in a variety of hematologic malignancies. Mesutoclax has an anti-tumor effect by selectively inhibiting BCL2 and restoring the mechanism of programmed cell death. Mesutoclax is the first BCL2 inhibitor to receive BTD recognition in China for the treatment of BTKi-treated mantle cell lymphoma.

The Phase I clinical trial of mesutoclax in combination with azacitidine for the first-line treatment of AML has been approved in the U.S. Updated data were presented in an oral presentation at the 2026 ASCO Annual Meeting.

As of April 13, 2026, among the evaluable TN AML patients, 81.8% achieved composite CR (cCR, CR+CRi). 86.5% were MRD (Minimal Residual Disease) negative.

Mesutoclax (ICP-248) is a novel, orally bioavailable BCL2 selective inhibitor developed by InnoCare. BCL2 is an important part of apoptotic pathway and is overexpressed in a variety of hematologic malignancies. Mesutoclax has an anti-tumor effect by selectively inhibiting BCL2 and restoring the mechanism of programmed cell death. The Phase I clinical trial of mesutoclax in combination with azacitidine for the treatment of MDS has been approved in the U.S. Updated data were presented in an oral presentation at the 2026 ASCO Annual Meeting.

As of April 20, 2026, among evaluable treatment-naïve (TN) MDS patients, the overall response rate (ORR) per IWG 2006 criteria was 100%, including complete response (CR) in 40%, and marrow CR in 60%. The composite CR rate was 90% per IWG 2023 criteria, including 60% CR.

ICP-B02 (CM355) is a CD20xCD3 bispecific antibody co-developed by InnoCare and Keymed. ICP-B02 binds to CD20 on the tumor cells and CD3 on the T cells, redirects and activates T cells to eradicate tumor cells through T-cell Directed Cellular Cytotoxicity (TDCC) in the treatment of CD20+ B-cell malignancies.

The preliminary data of both the intravenous infusion (IV) and the subcutaneous (SC) formulations have shown good efficacy of ICP-B02 in patients with follicular lymphoma (FL) and DLBCL.

In 2025, InnoCare and its partner out-licensed ICP-B02 to US firm Prolium (USD 520 million + minority equity stake).

NHLs are the main type of CD20+ B-cell malignancies, accounting for 80%-90%, which include DLBCL, follicular lymphoma (FL), MCL, and CLL/SLL.

Orelabrutinib, a novel BTK inhibitor developed by InnoCare, has high target selectivity, 100% BTK target occupancy rate and favorable PK profile, which make it suitable for the development and treatment of various autoimmune diseases. There are no BTK inhibitors for the treatment of primary immune thrombocytopenia (ITP) approved for marketing in China.  NDA for orelabrutinib for the treatment of patients with ITP has been accepted in China.

According to Phase II study results, both 50mg QD and 30mg QD of orelabrutinib were safe in the treatment of patients with ITP. 40% at the 50mg arm reached primary endpoint. 83.3% achieved durable response among patients met the primary endpoint. A subgroup analysis of patients who previously responded to glucocorticoids (GC) or intravenous immunoglobulin (IVIG) showed that 75.0% of patients at the 50mg dose achieved the primary endpoint. More data can be found in the oral presentation at the European Hematology Association (EHA) 2023 Hybrid Congress (abstract number: S299) and the article published at American Journal of Hematology.

ITP is an acquired immune mediated disorder characterized by a decrease in peripheral blood platelet counts, resulting in an increased risk of bruising and bleeding. The annual incidence rate of adult ITP is about 2-10 per 100,000 people. Only about 70% of patients respond to first-line treatment, which is still ineffective for some patients or relapse. Therefore, it is necessary to explore new therapeutic targets. Inhibiting BTK can inhibit B cell activation and autoantibody production, thereby reducing damage to platelets.

Orelabrutinib, a novel BTK inhibitor developed by InnoCare, has high target selectivity, 100% BTK target occupancy rate and favorable PK profile, which make it suitable for the development and treatment of various autoimmune diseases. Due to its excellent blood-brain barrier penetration, orelabrutinib has the potential to treat neurological diseases such as multiple sclerosis (MS). There are no BTK inhibitors for the treatment of MS approved for marketing in the world.

The global multicenter Phase II trial of orelabrutinib for the treatment of MS showed that the primary endpoint was achieved in all three treatment groups at week 24, and orelabrutinib significantly reduced disease activity in MS patients.

MS is an autoimmune, inflammatory disease of the central nervous system. If not diagnosed and treated in a timely manner, patients may experience paralysis, blindness, etc., and their quality of life is severely affected. According to Frost Sullivan analysis, it is estimated that the total number of MS patients worldwide will be 3.2447 million in 2025¹.

[1] https://www.chinabaogao.com/market/202112/562541.html

Orelabrutinib, a novel BTK inhibitor developed by InnoCare, has high target selectivity, 100% BTK target occupancy rate and favorable PK profile, which make it suitable for the development and treatment of various autoimmune diseases. Orelabrutinib the first BTK inhibitor to demonstrate significant efficacy in a Phase II clinical trial for SLE.  Currently, the Company has been accelerating the patient enrollment of the registrational Phase III clinical trial of orelabrutinib for the treatment of SLE. Orelabrutinib is expected to become a potential first-in class BTK inhibitor for the treatment of SLE.

Results from the Phase IIb clinical trial of orelabrutinib for SLE demonstrated that under stringent steroid-tapering requirements, orelabrutinib 75 mg once daily (QD) achieved a statistically significant improvement in SLE Response Index-4 (SRI-4) rate compared with placebo at Week 48 (57.1% vs. 34.4%, p = 0.01 vs placebo), meeting the primary endpoint. Mean cumulative corticosteroid exposure through 48 weeks was reduced by 301.0 mg in the 75 mg QD group versus placebo.

SLE is a systemic disease that often leads to damage to organs, especially the kidneys and nervous system, skin, blood system, respiratory system, and almost all systems may be affected. According to Frost Sullivan analysis, it is expected that there will be 8.18 million SLE patients worldwide by 2025. The Chinese Systemic Lupus Erythematosus Development Report 2020 points out that there are about one million SLE patients in China, ranking first in the world in number of patients and second in incidence rate.

TYK2 inhibitors for the treatment of atopic dermatitis (AD) approved for marketing in the world. Soficitinib was designed to be a potent and selective TYK2 inhibitor with 400 folds of selectivity against JAK2 to avoid the adverse events associated with nonselective JAK inhibitors.

Registrational phase III clinical study results of novel TYK2 (Tyrosine Kinase 2) inhibitor soficitinib (ICP-332) met the primary endpoint in patients with moderate-to-severe AD.

The study demonstrated that soficitinib achieved the primary endpoint with statistical significance and clinically meaningful improvement. In addition, multiple secondary endpoints were successfully met, demonstrating a consistent treatment effect across efficacy measures.

Soficitinib also showed a good safety profile, which was consistent with previous clinical studies, and no new safety signals were identified. Detailed efficacy and safety data from the study will be presented at upcoming international scientific congresses and/or academic journal.

According to the source of Pharma Intelligence, AD has become a major autoimmune disease with a global market potential of US$10 billion by 2030.

Soficitinib (ICP-332) is an oral TYK2 JH1 inhibitor developed by InnoCare. There are no TYK2 inhibitors for the treatment of atopic dermatitis (AD) approved for marketing in the world. Soficitinib was designed to be a potent and selective TYK2 inhibitor with 400 folds of selectivity against JAK2 to avoid the adverse events associated with nonselective JAK inhibitors.

Phase II portion of the Phase II/III trial of Soficitinib for non-segmental vitiligo has met the primary endpoint. Phase II results showed that, at Week 24, treatment with soficitinib resulted in significant improvements from baseline in Facial Vitiligo Area Scoring Index (F-VASI). The least-squares mean percent change from baseline in F-VASI was 38.8% in the 80 mg once-daily group and 41.2% in the 120 mg once-daily group, compared with 2.2% in the placebo group. The two soficitinib dose groups demonstrated statistically significant improvements versus placebo (P<0.0001).

Soficitinib also showed a favorable safety profile, which was consistent with previous clinical studies. The treatment was well tolerated, and no new safety signals were identified. Detailed efficacy and safety results will be presented at upcoming international scientific congresses and/or academic journal.

Soficitinib (ICP-332) is an oral TYK2 JH1 inhibitor developed by InnoCare. There are no TYK2 inhibitors for the treatment of atopic dermatitis (AD) approved for marketing in the world. Soficitinib was designed to be a potent and selective TYK2 inhibitor with 400 folds of selectivity against JAK2 to avoid the adverse events associated with nonselective JAK inhibitors. The global Phase II clinical trial of soficitinib for PN is progressing rapidly.

Soficitinib (ICP-332) is an oral TYK2 JH1 inhibitor developed by InnoCare. There are no TYK2 inhibitors for the treatment of atopic dermatitis (AD) approved for marketing in the world. Soficitinib was designed to be a potent and selective TYK2 inhibitor with 400 folds of selectivity against JAK2 to avoid the adverse events associated with nonselective JAK inhibitors.

CSU is characterized by recurrent wheals and itch, with a disease course typically lasting two to five years, and in some patients, even exceeding five years. China has a large population of CSU patients, a condition that is prone to recurrent episodes. The intense nighttime itching severely disrupts daily life. Long-term, systematic, and standardized treatment is therefore essential for disease control.

Soficitinib (ICP-332) is an oral TYK2 JH1 inhibitor developed by InnoCare. There are no TYK2 inhibitors for the treatment of atopic dermatitis (AD) approved for marketing in the world. Soficitinib was designed to be a potent and selective TYK2 inhibitor with 400 folds of selectivity against JAK2 to avoid the adverse events associated with nonselective JAK inhibitors.

Fadeucravacitinib (ICP-488) is a potent and selective TYK2 (tyrosine kinase 2) JH2 allosteric inhibitor developed by InnoCare. By binding the JH2 domain, fadeucravacitinib blocks the signal transduction of IL-23, IL-12, type 1 IFN and other inflammatory cytokine, thereby inhibiting the pathological process of autoimmune and inflammatory diseases.

Fadeucravacitinib (ICP-488) met the primary endpoint in the registrational Phase III clinical study in patients with moderate-to-severe plaque psoriasis. The study demonstrated that fadeucravacitinib achieved the primary endpoint with statistical significance and clinically meaningful improvement. In addition, multiple secondary endpoints were successfully met, demonstrating a consistent treatment effect across efficacy measures. Fadeucravacitinib also showed a favorable safety profile, which was consistent with previous clinical studies, and no new safety signals were identified.

Autoimmune diseases have become the third largest chronic disease after cardiovascular diseases and cancer. Data shows that 100 million people worldwide are affected by various types of psoriasis¹.

[1] Progress in Epidemiological Investigation of Psoriasis, Journal of Diagnostics Concepts & Practice. 2021.

Fadeucravacitinib (ICP-488) is a potent and selective TYK2 (tyrosine kinase 2) JH2 allosteric inhibitor developed by InnoCare. By binding the JH2 domain, fadeucravacitinib blocks the signal transduction of IL-23, IL-12, type 1 IFN and other inflammatory cytokine, thereby inhibiting the pathological process of autoimmune and inflammatory diseases.

Fadeucravacitinib (ICP-488) is a potent and selective TYK2 (tyrosine kinase 2) JH2 allosteric inhibitor developed by InnoCare. By binding the JH2 domain, fadeucravacitinib blocks the signal transduction of IL-23, IL-12, type 1 IFN and other inflammatory cytokine, thereby inhibiting the pathological process of autoimmune and inflammatory diseases.

ICP-538 is a novel, potent, highly selective, orally administered molecular glue degrader targeting VAV1,which is the first VAV1 degrader approved to enter clinical trials in China and the second globally.

ICP-538 induces rapid and efficient degradation of VAV1 protein in a dose-dependent manner by selectively mediating the formation of a ternary complex between the CRBN E3 ubiquitin ligase and the VAV1 protein. ICP-538 will be developed for the treatment of autoimmune diseases, such as inflammatory bowel disease, systemic lupus erythematosus, and multiple sclerosis. Currently, there are no approved VAV1-targeted therapies globally.

ICP-054 is a novel potentially best-in-class oral small molecule IL-17AA/AF inhibitor being developed by InnoCare in partnership with Zenas BioPharma. ICP-054 is designed to selectively block the signal transduction pathways of both the IL-17AA homodimer and IL-17AF heterodimer, inhibiting downstream pro-inflammatory cytokine and chemokine release.

Currently, no oral IL-17 inhibitors have been approved or are in late-stage development globally. ICP-054's oral, small molecule profile may offer meaningful advantages over currently approved biologic IL-17 therapies in terms of convenience, compliance, and accessibility.

Zenas BioPharma licensed the exclusive rights from InnoCare Pharma to develop, manufacture, and commercialize ICP-054 in all fields of use worldwide, excluding greater China and Southeast Asia.

Zurletrectinib, a pan-TRK inhibitor developed by InnoCare, markedly inhibits the activity of the wild type TRKA, TRKB and TRKC, as well as mutant TRKA with resistant mutation G595R or G667C. Zurletrectinib could overcome acquired resistance to the first generation TRK inhibitors.

Zurletrectinib has demonstrated good efficacy and safety profile with an overall response rate (ORR) of 80-90%, and was shown to overcome acquired resistance to the first generation TRK inhibitors, bringing hope for patients who failed prior TRKi therapy.

The Company is conducting clinical trial of zurletrectinib to treat pediatric patients (2 to 12 years old), adolescent patients (12 to 18 years old) and adult patients.

In some rare tumor types, such as congenital infantile fibrosarcoma, the incidence of NTRK gene fusion is as high as 90%. NTRK gene fusion is associated with at least 19 tumor types in adults and children, including lung cancer, colorectal cancer, breast cancer, pancreatic cancer and melanoma.

Zurletrectinib, a pan-TRK inhibitor developed by InnoCare, markedly inhibits the activity of the wild type TRKA, TRKB and TRKC, as well as mutant TRKA with resistant mutation G595R or G667C. Zurletrectinib could overcome acquired resistance to the first generation TRK inhibitors.

ICP-B794 is a novel ADC comprising a humanized anti-B7-H3 monoclonal antibody conjugated to potent in-house developed payload via a protease-cleavable linker. This combination ensures precise targeting of tumor cells while minimizing off-target effects, offering a promising treatment for solid tumors such as lung cancer, esophageal cancer, nasopharyngeal cancer, head and neck squamous cell carcinomas, prostate cancer, and others.

Currently, there are no B7-H3 targeted therapies approved for marketing globally. B7-H3 is a type I transmembrane protein that is highly expressed across multiple solid tumor types. Due to its tumor-specific expression, it is considered a highly promising anti-tumor target.

ICP-B208 is a novel ADC comprising a humanized anti-CDH17 monoclonal antibody conjugated to a potent, in-house invented payload via a protease-cleavable linker. This design enables significantly enhanced tumor-killing effects with improved stability and safety.

Currently, there are no approved CDH17 targeted ADCs globally.