On June 26, 2022 Innovent Biologics, Inc. ("Innovent") (HKEX: 01801), a world-class biopharmaceutical company that develops, manufactures and commercializes high-quality medicines for the treatment of cancer, autoimmune, metabolic, ophthalmology and other major diseases, and Eli Lilly and Company ("Lilly",NYSE: LLY), reported that the National Medical Products Administration (NMPA) of China has approved the supplemental New Drug Application (sNDA) for TYVYT (sintilimab injection) in combination with fluorouracil and platinum-based chemotherapy for the first-line treatment of unresectable, locally advanced, recurrent or metastatic gastric or gastroesophageal junction adenocarcinoma (Press release, Innovent Biologics, JUN 26, 2022, View Source [SID1234616257]).

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This is the sixth NMPA-approved indication of TYVYT. TYVYT is the first domestic PD-1 inhibitor approved for the first-line treatment of gastric cancer and is currently approved for the first-line treatment in five major types of cancers. In China, TYVYT was approved for the treatment of relapsed or refractory classical Hodgkin’s lymphoma in December 2018, first-line treatment of nonsquamous non-small cell lung cancer (NSCLC) in February 2021, first-line treatment of squamous NSCLC, and the first-line treatment of hepatocellular carcinoma in June 2021; and the first-line treatment of esophageal squamous cell carcinoma in June 2022.

The approval in China was based on the results of a randomized, double-blind, multicenter Phase III clinical trial (ORIENT-16, NCT03745170) evaluating sintilimab in combination with chemotherapy (oxaliplatin and capecitabine), compared to placebo in combination with chemotherapy, for the first-line treatment of unresectable, locally advanced, recurrent or metastatic gastric or gastroesophageal junction adenocarcinoma. Based on the interim analysis by Independent Data Monitoring Committee (iDMC), sintilimab in combination with chemotherapy demonstrated superior overall survival (OS), compared to placebo plus chemotherapy, with a 34.0% reduction in the risk of death (HR 0.660，95%CI 0.505-0.864，p=0.0023) and a 5.5-month improvement in median OS (mOS 18.4 months vs. 12.9 months) in patients with combined positive score (CPS) ≥5, and 23.4% reduction in the risk of death (HR 0.766, 95%CI 0.626-0.936，p=0.0090）and a 2.9-month improvement in mOS (15.2 months vs. 12.3 months) in all patients regardless of PD-L1 expression. The safety profile of sintilimab in this study was consistent with that observed in previously reported studies of sintilimab, and no additional safety signals were identified for the combination of sintilimab and chemotherapy. The results of ORIENT-16 study were presented at the European Society for Medical Oncology (ESMO) (Free ESMO Whitepaper) Congress 2021[1].

Prof. Jianming Xu, The Fifth Medical Center of People’s Liberation Army General Hospital stated: "Gastric cancer ranks fifth for global cancer incidence and is the third leading cause of cancer mortality worldwide[2]. Nearly half of global gastric cancer incidence cases and mortality cases occur in China annually[2]. The ORIENT-16 study demonstrated that sintilimab in combination with chemotherapy significantly prolonged overall survival of patients with gastric cancer[1]. We are encouraged by the approval of sintilimab, the first domestic anti-PD-1 monoclonal antibody approved for the treatment of gastric cancer, bringing a new and effective treatment option to be provided to patients with gastric cancer in China."

Dr. Yongjun Liu, President of Innovent, stated: "We are grateful for the recognition received from the Chinese regulatory authorities for TYVYT (sintilimab injection). This is the second sNDA approval this year, following the first one of ESCC, and enabling TYVYT (sintilimab injection) to be the domestically first innovative PD-1 inhibitor for the first-line treatment of five major type of cancers. We look forward to bringing TYVYT (sintilimab injection) as a new standard first-line treatment option for patients with advanced gastric cancer, and opening a new chapter of immunotherapy for gastric cancer. Innovent will uphold our mission of ‘to develop, manufacture and commercialize high-quality biopharmaceutical products that are affordable to ordinary people’ and make continuous contributions to the ‘Healthy China 2030’ implementation."

Dr. Hui Zhou, Senior Vice President of Innovent, stated, "The approval of TYVYT by the NMPA for the treatment of gastric cancer represents an important step forward for Innovent to further expand market coverage and is an important milestone for product development and commercial strategy. Data from the ORIENT-16 study demonstrated significant improvement in overall survival in patients with advanced gastric cancer and safety profile was consistent with that observed in previously reported studies of sintilimab. Survival benefit and reduction in the risk of death were observed, regardless of PD-L1 expression[1]. Gastric cancer is one of the most common malignancies in China and has different disease characteristics when compared with Western population. Innovent will continue to focus on these unmet medical needs and conduct additional clinical trials to untap the potential of our innovative molecules. We hope to bring more safe and efficacious treatment options to cancer patients both in China and worldwide."

Mr. Julio Gay-Ger, President and General Manager of Lilly China, stated, "China is well-known for gastrointestinal cancers[2]. The approval of TYVYT (sintilimab injection) as first-line treatment for gastric cancer marks another milestone. So far, TYVYT has covered major cancer types including lymphoma, lung cancer, liver cancer, esophageal cancer and gastric cancer, benefiting millions of Chinese patients. With our commitment to oncology, Lilly strives for bringing high-quality and affordable innovative drugs to Chinese cancer patients through both independent R&D and local partnerships. We look forward to continually working with our partner Innovent in bringing more innovative anti-tumor drugs to Chinese patients."

Dr. Li Wang, Senior Vice President of Lilly China and Head of Lilly China Drug Development and Medical Affairs Center, stated, "The ORIENT-16 study, led by Chinese investigators, is the first randomized, double-blind Phase III clinical study in China to demonstrate the significant benefit of immunotherapy combined with chemotherapy for the first-line treatment of advanced gastric cancer[1]. It provided strong evidence for the treatment of advanced gastric cancer in China. The approval of TYVYT (sintilimab injection) as first-line treatment for gastric cancer has provided a new option and fresh perspective for existing treatment, and will further benefit more and more Chinese gastric patients"

About the ORIENT-16 Study

ORIENT-16 is a randomized, double-blind, multi-center Phase 3 clinical study evaluating sintilimab or placebo, in combination with chemotherapy (oxaliplatin and capecitabine), for the first-line treatment of unresectable, locally advanced, recurrent or metastatic gastric or gastroesophageal junction (G/GEJ) adenocarcinoma (ClinicalTrials.gov, NCT03745170). The primary endpoint was overall survival, in PD-L1 positive (CPS>5) and all randomized patients[1].

As of the cutoff date for the interim analysis, a total of 650 patients were enrolled and randomly assigned with a 1:1 ratio to receive sintilimab or placebo in combination with chemotherapy until disease progression, unacceptable toxicity, withdrawal of consent, or death, whichever occurs first. The study met both primary endpoints and the safety profile of sintilimab in this study was consistent with that observed in previously reported studies of sintilimab, and no additional safety signals were identified for the combination of sintilimab and chemotherapy. The results were published at the ESMO (Free ESMO Whitepaper) Congress 2021.

About Gastric Cancer

Gastric cancer is one of the most common malignant tumor types worldwide. According to GLOBOCAN estimates, there were approximately one million new cases in 2020 and 769,000 new deaths of gastric cancer each year, making it the fifth most common cancer and third leading cause of cancer death globally[2],[3]. About half of all gastric cancer cases occurred in East Asia, mainly in China[2]. The first-line treatment of advanced gastric cancer is still limited. Currently, the 5-year survival rate of advanced or metastatic gastric cancer ranges from 5 to 20 percent. The median survival was about 1 year for patients who received chemotherapy only[4],[5].

About Sintilimab

Sintilimab, marketed as TYVYT (sintilimab injection) in China, is a PD-1 immunoglobulin G4 monoclonal antibody jointly developed by Innovent and Eli Lilly and Company. Sintilimab is a type of immunoglobulin G4 monoclonal antibody, which binds to PD-1 molecules on the surface of T-cells, blocks the PD-1 / PD-Ligand 1 (PD-L1) pathway, and reactivates T-cells to kill cancer cells[6]. Innovent is currently conducting more than 20 clinical studies of sintilimab to evaluate its safety and efficacy in a wide variety of cancer indications, including more than 10 registrational or pivotal clinical trials.

In China, sintilimab has been approved for six indications as below, with the first four included in the National Reimbursement Drug List (NRDL), including:

The treatment of relapsed or refractory classic Hodgkin’s lymphoma after two lines or later of systemic chemotherapy;
In combination with pemetrexed and platinum chemotherapy, for the first-line treatment of non-squamous non-small cell lung cancer lacking EGFR or ALK driver mutations;
In combination with gemcitabine and platinum chemotherapy, for the first-line treatment of squamous non-small cell lung cancer;
In combination with BYVASDA (bevacizumab biosimilar injection) for the first-line treatment of unresectable or advanced hepatocellular carcinoma;
In combination with cisplatin plus paclitaxel or cisplatin plus 5-fluorouracil for the first-line treatment of esophageal squamous cell carcinoma;
In combination with fluorouracil and platinum-based chemotherapy for the first-line treatment of unresectable, locally advanced, recurrent or metastatic gastric or gastroesophageal junction adenocarcinoma.
Innovent currently has the regulatory submission for sintilimab in combination with bevacizumab biosimilar and chemotherapy for EGFR-mutated non-squamous NSCLC following EGFR-TKI treatment under review in the China’s NMPA.

Additionally, two clinical studies of sintilimab have met their primary endpoints:

Phase 2 study as second-line treatment of esophageal squamous cell carcinoma;
Phase 3 study as second-line treatment for squamous NSCLC with disease progression following platinum-based chemotherapy.

On June 26, 2022 Antengene Corporation Limited ("Antengene" SEHK: 6996.HK), a leading innovative, commercial-stage global biopharmaceutical company dedicated to discovering, developing and commercializing first-in-class and/or best-in-class therapeutics in hematology and oncology, reported that it has entered into a clinical trial collaboration with BeiGene to evaluate the safety, pharmacokinetics, pharmacodynamics and preliminary efficacy of selinexor in combination with BeiGene’s anti-PD-1 checkpoint inhibitor, tislelizumab (Press release, Antengene, JUN 26, 2022, View Source [SID1234616256]). This multi-center, open-label Phase I/II trial will evaluate the investigational combination as a potential treatment option for patients with T and NK-cell lymphoma.

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"We are delighted to partner with BeiGene, a company that strives for innovation and excellence, and is committed to developing best-in-class or first-in-class anti-cancer therapies for patients across the globe. These qualities are very similar to those of our vision at Antengene," said Dr. Jay Mei, Antengene’s Founder, Chairman and CEO. "We look forward to advancing the combination of selinexor and tislelizumab to clinical development. With good data we will be able to bring this treatment regimen to patients with T and NK-cell lymphoma, diseases that are endemic in Asia but underserved by current therapies."

"At Antengene, we believe that the combinational use of immuno-oncology drugs and Selective Inhibitor of Nuclear Export (SINE) compounds possesses huge potential as novel treatment regimens for cancer patients," said Dr. Kevin Lynch, Antengene’s Chief Medical Officer. "The mechanism of action of selinexor in inhibiting the nuclear export protein XPO1 facilitates the intranuclear accumulation of tumor suppressors, making it a good partner in multiple combination treatment regimens. Preclinical research we conducted demonstrated that selinexor combined with a checkpoint inhibitor increased anti-tumor activity in multiple tumor models. In addition, deep and durable responses were also seen in multiple case reports of patients with T and NK-cell lymphoma treated with selinexor in combination with an anti-PD-1 checkpoint inhibitor. We hope to confirm that selinexor can synergize with tislelizumab to deliver an effective treatment regimen and help address the huge unmet medical needs in T and NK-cell lymphoma in the Asia Pacific regions and around the world." continued Dr. Lynch.

Tislelizumab is a PD-1 inhibitor designed to help aid the body’s immune cells to detect and fight tumors. Tislelizumab, a humanized monoclonal antibody, is specifically designed to minimize binding to FcγR on macrophages. In pre-clinical studies, binding to FcγR on macrophages has been shown to compromise the anti-tumor activity of PD-1 antibodies through activation of antibody-dependent macrophage-mediated killing of T effector cells.

About T and NK-Cell Lymphoma

T and NK-cell lymphoma is a set of heterogeneous diseases, accounting for 25-30% of Non-Hodgkin Lymphoma (NHL) cases in China and only about 10% in USA and Europe. There has been little improvement in the past decade when compared to B-cell Non-Hodgkin Lymphoma (B-NHL) as 5-year overall survival rate was only 30% in most common subtypes[1]. The unmet medical needs remain as agents with new mechanism of action to be explored and possibility to improve the treatment paradigm for the disease.

About the SINE Compounds

Selective Inhibitor of Nuclear Export (SINE) compounds are inhibitors of the major nuclear export protein Exportin 1 (XPO1). Currently, there are three oral SINE compounds, ATG-010 (selinexor), ATG-016 (eltanexor), and ATG-527 (verdinexor), under clinical development. Antengene has obtained exclusive development and commercialisation rights from Karyopharm Therapeutics Inc. (Nasdaq: KPTI) to these three compounds in certain APAC markets.

About XPOVIO (Selinexor)

XPOVIO is the world’s first approved orally-available, selective inhibitor of the nuclear export protein XPO1. It offers a novel mechanism of action, synergistic effects in combination regimens, fast onset of action, and durable responses.

By blocking the nuclear export protein XPO1, XPOVIO can promote the intranuclear accumulation and activation of tumor suppressor proteins and growth regulating proteins, and down-regulate the levels of multiple oncogenic proteins. XPOVIO delivers its antitumor effects through three mechanistic pathways: 1) exerting antitumor effects by inducing the intranuclear accumulation of tumor suppressor proteins; 2) reducing the level of oncogenic proteins in the cytoplasm by inducing the intranuclear accumulation of oncogenic mRNAs; and 3) restoring hormone sensitivity by activating the glucocorticoid receptors (GR) pathway. To utilize its unique mechanism of actions, XPOVIO is being evaluated for use in multiple combination regimens in a range of indications. At present, Antengene is conducting 10 clinical studies of XPOVIO in mainland China for the treatment of relapsed/refractory hematologic malignancies and solid tumors (3 of these studies are being jointly conducted by Antengene and Karyopharm Therapeutics Inc. [Nasdaq:KPTI]).

XPOVIO is approved in South Korea for two indications:

In combination with dexamethasone for the treatment of adult patients with relapsed or refractory multiple myeloma (R/R MM) who have received at least four prior therapies and whose disease is refractory to at least two proteasome inhibitors, at least two immunomodulatory agents, and an anti-CD38 monoclonal antibody.
As a monotherapy for the treatment of adult patients with relapsed or refractory diffuse large B-cell lymphoma (R/R DLBCL), not otherwise specified, including DLBCL arising from follicular lymphoma, after at least 2 lines of systemic therapy.
XPOVIO is approved in mainland China for one indication:

In combination with dexamethasone for the treatment of adult patients with relapsed or refractory multiple myeloma (R/R MM) who have received prior therapies and whose disease is refractory to at least one proteasome inhibitor, at least one immunomodulatory agent, and an anti-CD38 monoclonal antibody.
XPOVIO is approved in Australia for two indications:

In combination with bortezomib and dexamethasone (XVd) for the treatment of adult patients with multiple myeloma (MM) who have received at least one prior therapy.
In combination with dexamethasone (Xd) for the treatment of adult patients with relapsed or refractory multiple myeloma (R/R MM) who have received at least three prior therapies and whose disease is refractory to at least one proteasome inhibitor (PI), at least one immunomodulatory agent (IMiD), and an anti-CD38 monoclonal antibody (mAb).
XPOVIO is approved in Singapore for three indications:

In combination with bortezomib and dexamethasone for treatment of adult patients with multiple myeloma (MM) who have received at least one prior therapy.
In combination with dexamethasone for the treatment of adult patients with relapsed or refractory multiple myeloma (R/R MM) who have received at least four prior therapies and whose disease is refractory to at least two proteasome inhibitors, at least two immunomodulatory agents, and an anti-CD38 monoclonal antibody.
As a monotherapy for the treatment of adult patients with relapsed or refractory diffuse large B-cell lymphoma (R/R DLBCL), not otherwise specified, including DLBCL arising from follicular lymphoma, after at least 2 lines of systemic therapy who are not eligible for haematopoietic cell transplant.

On June 25, 2022 Dragon Boat reported that its IND application of the innovative anti-CLDN 18.2/CD47 bi-specific antibody (bsAb) injection (R&D code: BC007) was officially accepted by National Medical Products Administration (NMPA) under the acceptance number CXSL2200267 (Press release, Dragonboat Biopharmaceutical, JUN 25, 2022, View Source [SID1234616258]). This drug is the first domestic clinical filing of the CLDN 18.2/ CD47 bsAb, which is intended for the treatment of late stage solid tumors.

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BC007 is a innovative bsAb targeting CLDN 18.2 and CD47 and the early-stage development was completed collaboratively by Sanyou and Dragon Boat. Validation results of the in vivo efficacy showed that BC007 exhibited dose-dependent anti-tumor effects against CLDN18.2 overexpressing CDX mouse models of human gastric cancer, human pancreatic cancer and human colon cancer, and was significantly better than the selected comparator antibody. In the safety studies, hematological toxicity is one of the common challenges of CD47 targeting antibodies. But in the cynomolgus monkey toxicity study, multiple doses of BC007 was administered for 5 weeks without animal death, and the hematological toxicity was mild and well tolerated by the animals.

In March this year, the IND application of anti-CLDN 18.2 antibody injection (BC008) developed by Dragon Boat has been approved by National Medical Products Administration. In the future, Dragon Boat will bring greater clinical benefits to the patients by exploring more treatment options.

Dr. Guojun Lang, CEO of Sanyou, said "We sincerely congratulate Dragon Boat on the NMPA acceptance of IND application with the CLDN 18.2/CD47 bsAb, which is another milestone after the clinical approval of the anti-CLDN 18.2 nanoantibody co-developed by Sanyou and Dragon Boat in March. This project further proves the outstanding competency of Dragon Boat in the field of innovative biopharmaceutical research and development. This project is also another successful case of Sanyou’s Cooperative Project Organization (CPO) business model. We wish the clinical studies will proceed successfully and benefit the patients as soon as possible".

About CLDN 18.2

Tight junction protein claudin-18 isoform 2 (CLDN18.2) is a member of the claudin family, which includes tight junction proteins that establish paracellular barriers to control the molecular passage and motions among cells. Normally, CLDN 18.2 is expressed only on the surface of differentiated epithelial cells of the gastric mucosa. However, after the development of malignant tumors, tight junction proteins are disrupted, exposing the CLDN 18.2 epitope on the surface of tumor cells. Studies have shown high CLDN 18.2 expression in the tumor cells of 50%-80% of gastric cancer patients and 60% of pancreatic cancer patients.

About CD47

CD47 is a glycosylated transmembrane protein, a key member of the immunosuppressive signaling pathway, which inhibits macrophage phagocytosis and mediates the immune escape mechanism of various malignant tumors, mainly by interacting with the inhibitory receptor signal-regulatory protein alpha (SIRPα), which is widely recognized as a "don’t eat me" signal. Numerous studies have shown that CD47 is overexpressed in different types of tumors, including myeloma, smooth muscle sarcoma, acute lymphoblastic leukemia, and non-Hodgkin’s lymphoma.

On June 24, 2022 Genor Biopharma (Stock code: 6998.HK) reported that the company has entered into a cooperative development agreement (the "Cooperative Development Agreement") with Suzhou Abogen Biosciences Co., Ltd ("Abogen") to jointly develop globally innovative mRNA products and related pharmaceuticals (Press release, Genor Biopharma, JUN 24, 2022, View Source [SID1234616255]).

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According to the Cooperative Development Agreement, the Group’s biological antibody development platform will be integrated with Abogen’s mRNA technology platform to enable the Group and Abogen to jointly research and develop mRNA drugs for tumor treatment.

As an innovative, platform and integrated company with the ability to carry out innovative medical research and development, preclinical research, clinical development, registration, Chemistry, Manufacturing and Controls (CMC) development and commercialised manufacturing, the Company strives to develop globally innovative advantageous products with patents around the world. At present, the Company has successfully established the global first-in-class ("FIC")/ best-in-class ("BIC") differential research and development platform for early identifying bi-specific/multi-specific antibodies in immune-oncology. Innovation and exploration of FIC/BIC potential have been conducted in multi-dimension based on the in-depth understanding of our research and development team regarding targeted antibody molecular biology, cell biology and immunological mechanisms. To date, a number of projects for discovering bi-specific/multi-specific antibodies with FIC/BIC potential have been initiated. The Company is optimistic about the prospects of the application of mRNA technology in the pharmaceutical field. Through this cooperation, the Company expects to fully leverage the Company’s early exploration of highly differential FIC/BIC potential and the advantages of the respective platforms of both parties to accelerate the exploration and research and development of potential mRNA drugs for tumor treatment.

On June 24, 2022 Bold Therapeutics, a clinical-stage biopharmaceutical company, reported that they will be attending the Metals in Medicine Gordon Research Conference focusing on Advancing the Use of Metal-Based Compounds and Nanotheranostics for Personalized Medicine (Press release, Bold Therapeutics, JUN 24, 2022, View Source [SID1234616254]). The conference will be held in Andover, New Hampshire from June 26 to July 1, 2022, bringing together over 150 academic, industry, and government experts.

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Adam Carie, Director of CMC & Nonclinical Development, will be presenting on behalf of Bold Therapeutics in the "Clinical Advances for Metals in Medicine" session. He is joined by Shane Harrypersad, Senior Scientist, CMC.

This presentation will include previously embargoed data (shown below) recently presented at the 2022 American Society of Cancer Oncology (ASCO) (Free ASCO Whitepaper) Annual Meeting in a session entitled "BOLD-100-001 (TRIO039): A Phase 1b dose-escalation study of BOLD-100 in combination with FOLFOX chemotherapy in patients with advanced gastrointestinal solid cancers: Interim safety, tolerability, and efficacy." In addition to demonstrating that BOLD-100 was safe and generally well-tolerated, this data showed remarkable outcomes in the treatment of 3rd line or later treatment-resistant metastatic colorectal cancer (mCRC) in combination with FOLFOX – including in patients that had previously failed on FOLFOX alone. In the initial six patients, Progression-Free Survival (PFS) significantly exceed expected PFS for this patient population, handily exceeding the current best-in-class approved therapies for 3rd line mCRC, Bayer’s Stivarga (regorafenib) and Taiho’s Lonsurf (trifluridine and tipiracil).

While only the earliest efficacy data from the Phase 1b portion of the study was available for presentation at ASCO (Free ASCO Whitepaper), the colorectal arm of the BOLD-100-001 Phase 2 trial has since fully enrolled (N=22) and Bold Therapeutics expects to announce additional efficacy data in mCRC by year-end.

Bold Therapeutics’ BOLD-100 is a first-in-class ruthenium-based small molecule therapeutic that (1) alters the unfolded protein response (UPR) through selective GRP78 inhibition; and (2) induces reactive oxygen species (ROS) which causes DNA damage and cell cycle arrest. Collectively, these effects result in cell death in both sensitive and resistant cancers, giving BOLD-100 the potential to significantly improve outcomes in a wide range of both solid and liquid tumors in combination with other anticancer therapies ranging from traditional chemotherapies to targeted therapies to immuno-oncology agents. BOLD-100 is currently being studied in a multinational Phase 2 trial in the treatment of advanced gastrointestinal cancers actively enrolling at 13 clinical sites: six in Canada; two in the U.S.; and five in South Korea.

"Bold Therapeutics is excited to present these remarkable results at the Gordon Research Metals in Medicine Conference showcasing the cutting-edge, multi-disciplinary work being performed at Vancouver-based Bold Therapeutics" noted Dr. Carie. "With our Phase 2 clinical trial well underway at sites in Canada, the United States, and South Korea, we are excited to connect with other leaders in the development of metal-based oncology therapeutics with a goal of improving outcomes for patients. With unique expertise in metallochemistry and manufacturing, translational research and rapid and efficient early-stage clinical development, Bold Therapeutics is actively seeking additional preclinical-stage metal-based therapeutics to in-license, develop and commercialize."

In parallel, Bold Therapeutics is actively seeking global development partners to support two additional parallel Phase 2 studies: (1) BOLD-100 in combination with a proteasome inhibitor (e.g. Takeda’s Velcade (bortezomib) or Amgen’s Kyprolis (carfilzomib)) in the treatment of multiple myeloma; and (2) BOLD-100 in combination with a standard-of-care agent in the treatment of bladder cancer. Compelling preclinical data supporting these development initiatives is available under confidentiality.