InnoCare Pharma (HKEX: 09969), a leading biopharmaceutical company focusing on cancer and autoimmune diseases, today announced 2021 annual results as of 31 December 2021.

Dr. Jasmine Cui, Co-founder, Chairwoman and CEO of InnoCare, said, “We are delighted to announce 2021 results on the occasion of our 2nd anniversary of listing on Hong Kong,China, Stock Exchange. We have witnessed an unusual year 2021, in which we overcame tremendous difficulties and challenges and achieved many significant milestones. We have achieved satisfactory results in the first year of commercialization. The inclusion of orelabrutinib in the National Reimbursement Drug List (NRDL) at the end of 2021 will help access to more patients. We have made major breakthroughs in internationalization by reaching license-out and license-in collaboration with Biogen and Incyte respectively. We have deepened our efforts in innovation and accelerated the progress of our global multicenter clinical trials so as to further advance our drug candidate to benefit more patients…”

Financial Highlights

?    The revenue increased sharply from 1.4 million for the year ended 31 December 2020 to 1.043 billion for the year ended 31 December 2021, due to sales of orelabrutinib and upfront payment from Biogen.

?    The research and development expenses increased from 402.8 million for the year ended 31 December 2020 to 721.6 million for the year ended 31 December 2021, primarily due to the upfront payment of tafasitamab license-in, etc.

?    The cash and cash equivalent increased from 3.9696 billion by the end of 2020 to 6.5505 billion by the end of 2021.

?    The loss for the reporting period decreased from 391.9 million for the year ended 31 December 2020 to 66.7 million for the year ended 31 December 2021, mainly due to the increase of revenue, etc.

(Note: Currency: RMB)

Key Highlights and Milestones

Bruton's tyrosine kinase (BTK) inhibitor orelabrutinib

?    Commercial achievements

InnoCare successfully launched the first prescription of orelabrutinib in mid-January 2021. InnoCare’s commercial team about 250 experienced members rapidly covered over 1000 leading hospitals in more than 260 cities all over China by the end of 2021, generating a gross revenue of RMB 241 million.

 In December 2021, orelabrutinib was included in China’s NRDL to help access to more patients in 2022 and beyond.

?    Business development

In September 2021, InnoCare received the upfront payment of US$ 125 million from Biogen based on the license-out agreement for orelabrutinib for the potential treatment of multiple sclerosis (MS). In addition, InnoCare is eligible to receive up to US$ 812.5 million in potential development milestones and commercial payments should the collaboration achieve certain development and commercial milestones. The Company is also eligible to receive a tiered royalties in the low to high teens percentage rate on potential future net sales resulting from the collaboration.

Currently, the global Phase II trial for MS is ongoing in US, Europe and China.

?    R&D development

Orelabrutinib for the treatment of Systemic Lupus Erythematosus (SLE)

Orelabrutinib Phase II trial for the treatment of SLE was completed at the end of 2021.

The Phase II results showed that oral orelabrutinib was safe and well tolerated in patients with mild to moderate SLE. A dose-dependent efficacy was observed in all treated evaluable patients. The SLE Responder Index (SRI)-4 response rates at 12-week were 35.7%, 50.0%, 61.5% and 64.3% in patients treated with placebo, 50 mg/day, 80 mg/day and 100 mg/day of orelabrutinib respectively.

Treatment with orelabrutinib led to a reduction in levels of proteinuria, and improvements of immunologic markers, including reduced immunoglobulin G, increased complements C3 and C4.

Further clinical development of orelabrutinib in SLE patient is warranted and planned.

Orelabrutinib for the first-line treatment of MCD DLBCL

A Phase III, randomized, double-blind, placebo-controlled, multicenter study evaluating the efficacy and safety of orelabrutinib plus R-CHOP versus placebo plus R-CHOP in first-line treatment of patients with MCD subtype diffuse large B-cell lymphoma (DLBCL) is ongoing.

ICP-B04 (Tafasitamab)

?    In August 2021, InnoCare entered into a Collaboration and License Agreement with Incyte for the development and commercialization of tafasitamab, a humanized Fc-modified cytolytic CD-19 targeting monoclonal antibody, in Greater China. Tafasitamab in combination with lenalidomide was approved by the U.S. Food and Drug Administration (FDA) and European Medicines Agency for the treatment of eligible patients with relapsed or refractory (R/R) DLBCL.

?    The strategic collaboration with Incyte will not only offer a good opportunity to explore the potential clinical benefit to combine tafasitamab with orelabrutinib and InnoCare’s other assets for the treatment of B-cell malignancy, but also enhance InnoCare’s strength in the field of hematology and oncology.

?    Tafasitamab in combination with lenalidomide was approved by the Health Commission and Medical Products Administration of Hainan Province, under the early access program in Boao Lecheng International Medical Tourism Pilot Zone for the treatment of eligible DLBCL patients.

ICP-192 (Gunagratinib)

Gunagratinib is currently undergoing several Phase I/II clinical studies in China and the U.S. In China, in the dose-escalation part of Phase I/II trial, gunagratinib demonstrated safe and well-tolerated profile across all dosage cohorts ranging from 2 to 26 mg with no dose-limiting toxicities (DLT) observed.

?    Head and neck cancer

In the dose-escalation trial, anti-tumor activity of gunagratinib was observed in head and neck cancer patients carrying FGF/FGFR gene aberrations. Among nine patients with FGF/FGFR gene aberrations who have completed at least one tumor assessment, the overall response rate (ORR) was 33.3%.

At the beginning of 2022, InnoCare initiated a clinical trial of basket solid tumors focusing on head and neck cancer patients with FGF/FGFR gene aberrations.

?    Cholangiocarcinoma

In the Phase II trial, 20mg gunagratinib showed preliminary efficacy in cholangiocarcinoma patients. As of 13 January 2022, among the patients who have completed at least one tumor assessment, the ORR was 60.0%. The disease control rate (DCR) was 100%.

?    International progress

In June 2021, gunagratinib was granted the Orphan Drug Designation for the treatment of cholangiocarcinoma by the U.S. FDA. In the U.S. and Australia, Phase I/II dose escalation trial in cholangiocarcinoma and head & neck cancer is ongoing.

ICP-723

?   As of 11 February 2022, a total of 17 patients in Phase I dose escalation trial were treated with ICP-723 at doses of 1 mg to 8 mg once daily. ICP-723 was safe and well tolerated with no DLT observed. Five of 17 patients were considered as NTRK gene fusion positive. Among the five patients, the ORR was 80%, and the DCR was 100%. The ORR was 100% in dose groups of 4mg and above.

?   In the U.S., InnoCare got the IND clearance in August 2021 for the treatment of NTRK fusion positive cancers and will start the Phase I clinical trial in the U.S. in 2022.

ICP-332

?     ICP-332 is developed for the treatment of various autoimmune disorders. The Phase I clinical trial of the novel tyrosine kinas 2 (TYK2) inhibitor was completed. ICP-332 demonstrated dose proportionality of the PK parameters in the range of 5 mg to 320 mg. No significant food effect was observed. ICP-332 was safe and well tolerated and the maximum tolerated dose was not reached.

?     ICP-332 also avoided certain adverse effects associated with non-selective JAK inhibitors.

ICP-B05 (newly disclosed)

?     ICP-B05 is an anti-CC chemokine receptor 8 (CCR8) monoclonal antibody, a potential first-in-class drug co-developed by InnoCare and KeyMed as a monotherapy or in combination with other therapies for the treatment of various cancers.

?     CCR8 has been shown to be selectively overexpressed on immunosuppressive regulatory T cells (Tregs) in tumor microenvironment (TME). ICP-B05 binds to CCR8 on Tregs and eradicates immunosuppressive Tregs through ADCC to augment the anti-tumor immunity in TME while preserving peripheral homeostasis. ICP-B05 has the potential to deliver optimal tumor targeted Treg depletion and be more specific in anti-tumor activity than other immunotherapies.

?     IND application is expected to be submitted in the second quarter of 2022.

By now, InnoCare has built a robust pipeline. In addition to the two approved indications, InnoCare is conducting additional six registrational trials with orelabrutinib. Besides, there are nine clinical stage assets and multiple other IND enabling stage candidates. Over 30 clinical trials are ongoing globally.

Orelabrutinib’s Other Clinical Development

Liguid Cancer

Orelabrutinib was included in the 2021 CSCO Diagnosis and Treatment Guidelines for Malignant Lymphoma and is recommended as a Class I treatment for R/R chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL) and R/R mantle cell lymphoma (MCL).

?    R/R WM: The New Drug Application (NDA) for R/R waldenstrom’s macroglobulinemia (WM) was accepted by Center for Drug Evaluation (CDE) in March 2022.

?    R/R MZL: A multicenter, open-label study to evaluate the safety and efficacy of orelabrutinib in patients with R/R marginal zone lymphoma (MZL) is ongoing. The NDA for R/R MZL is expected to be submitted in China in the first half of 2022.

?    R/R CLL/SLL: At the 63rd American Society of Hematology (ASH) Annual Meeting, orelabrutinib showed a significant higher CR/CRi (complete response / incomplete marrow recovery) rate in R/R CLL/SLL in comparison with other BTK inhibitors at a similar median follow-up period with ORR of 93.8% and CR/CRi of 26.3%.

?    R/R MCL: In the U.S., a Phase II registrational trial for R/R MCL is expected to complete patient enrollment in 2022. In June 2021, U.S. FDA granted Breakthrough Therapy Designation (BTD) to orelabrutinib for the treatment of R/R MCL.

?    1L CLL/SLL: A Phase III registrational trial for first-line treatment of CLL/SLL is conducted in China, comparing orelabrutinib monotherapy versus rituximab plus chlorambucil. It is expected to finish the patient enrollment in 2023.

?    1L MCL: In China, a Phase III registrational trial for first-line treatment of MCL is conducted, comparing orelabrutinib in combination with R-CHOP versus R-CHOP.

?    InnoCare is exploring the combinational therapy of orelabrutinib with obinutuzumab (Gazyva), an anti-CD20 antibody, for the treatment of B cell lymphoma.

Autoimmune Diseases

In addition to the above-mentioned updates of orelabrutinib in MS and SLE, InnoCare is also exploring orelabrutinib for the treatment of primary immune thrombocytopenia purpura (ITP) and neuromyelitis optica spectrum disorder (NMOSD).

?    ITP: The IND application for orelabrutinib for the treatment of ITP was approved by CDE in August 2021 and the first patient of the Phase II clinical trial was dosed in China in February 2022.

?    NMOSD: In February 2022, InnoCare received the IND approval of orelabrutinib by NMPA for starting Phase II clinical trial in NMOSD in China.

Highlights of Other Pipeline Projects

Liquid Cancer

?     ICP-B02 (CM355): A CD20xCD3 bispecific antibody co-developed by InnoCare and KeyMed for the treatment of lymphoma. In preclinical studies, it demonstrated stronger T-cell-dependent cellular cytotoxicity (TDCC) activities with less cytokine release. The dosing of the first patient was completed in January 2022.

?     ICP-490: A highly potent orally bioavailable next-generation CRBN modulator that modulates the immune system and other biological targets. The IND application is expected to be submitted in the first half of 2022.

?     ICP-248: A novel, orally bioavailable B cell lymphoma-2 (BCL-2) selective inhibitor. It can be developed in combination with orelabrutinib for hematological malignancies. The IND application for ICP-248 will be submitted in China in the first half of 2022.

Solid Tumor

?     ICP-189: A potent oral allosteric inhibitor of SHP2 (Src Homology 2 domain containing protein tyrosine phosphatase) developed for the treatment of solid tumors as a cornerstone therapy in combinations with other antitumor agents. InnoCare has received the IND approval of ICP-189 from the NMPA in October 2021 and the IND clearance of ICP-189 by the U.S. FDA for starting clinical trial in the U.S. in November 2021.

?     ICP-033: A novel multi-target Receptor Tyrosine Kinase (RTK) inhibitor, which will be used potentially as monotherapy and/or in combination with immunotherapy and other targeted drugs to treat liver cancer, renal cell carcinoma, colorectal cancer and other solid tumors. The IND application for ICP-033 was approved by the CDE in June 2021 and Phase I clinical trial is ongoing.

?     ICP-915: A highly potent, selective small-molecule inhibitor against the G12C mutant form of Kirsten Rat Sarcoma (KRAS) viral oncogene homologue. It will be developed in combination with ICP-189 to treat various types of solid tumors.

?     ICP-B03: A tumor-conditional pro-interleukin-15 (IL-15) targeting and changing immune cells inside tumor microenvironment. IL-15 is a cytokine that stimulates important anti-tumor immune cells, such as CD8+T cells and Natural Killer (NK) cells.

Autoimmune Diseases

?     ICP-488: A potent and selective TYK2 allosteric inhibitor, binding to the TYK2 JH2 domain, developed for the treatment of inflammatory diseases such as psoriasis and inflammatory bowel disease (IBD). The CDE has approved the clinical trial of ICP-488 in March 2022.

Other Corporate Development

?    Financing

In February 2021, InnoCare brought in Hillhouse as a strategic investor and Vivo Capital increased its shareholdings, raising a funding of US$393 million;

From December 2021 to January 2022, two substantial shareholders of InnoCare purchased an aggregate of about 13 million shares of the Company through on-market transactions;

In September 2021, InnoCare’s application for listing on the STAR Board of Shanghai Stock Exchange was accepted.

?    Manufacturing

Guangzhou: InnoCare Guangzhou has completed Phase I project covering 50,000 square meters by the end of 2020 and obtained a drug manufacturing license for the facility. InnoCare Guangzhou also finished the technology transfer process from its CMO and is ready for orelabrutinib commercial production in the first half of 2022.

Beijing: At the end of 2021, InnoCare obtained a land of over 70,000 square meters in Beijing next to the Company’s headquarter inside the Life Science Park to build a landmark R&D center and large molecule production facility. Currently, InnoCare has finished the conceptional design and expect the construction to be completed in 2025.

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?    Talent

Dr. Sean Zhang and Dr. Davy Ouyang joined InnoCare as Chief Medical Officer and Biology Vice President, respectively, in the first half of 2021,

Mr. Nan Gao and Ms. Jessie Wang joined InnoCare as Chief Operation Officer and General Counsel, respectively, in the second half of 2021.

“Looking forward into 2022, we will continue our hard-work to further enhance our R&D strength, accelerate clinical trials, improve commercialization capabilities, bring in more international business development opportunities... so as to propel the Company to a new level,” added Dr. Cui.

To know more about the detailed financial data and business update of InnoCare 2021 annual results, please log in https://cn.innocarepharma.com/en/investor-relations/ .

Conference Call Information

InnoCare will host a conference call on March 23, 2022 at 9:00 a.m. Beijing time. Participants must register in advance of the conference call. Details are as follows:

Registration Link: https://goldmansachs.zoom.us/webinar/register/WN_JKhYhUVYS1W8HrlfBjzWsg

The call will be conducted in Mandarin.

About InnoCare

InnoCare is a commercial stage biopharmaceutical company committed to discovering, developing, and commercializing first-in-class and/or best-in-class drugs for the treatment of cancer and autoimmune diseases. We strategically focus on lymphoma, solid tumors, and autoimmune diseases with high unmet medical needs in China and worldwide. InnoCare has branches in Beijing, Nanjing, Shanghai, Guangzhou, Hong Kong,China, New Jersey and Boston.