Sanyou Biopharmaceuticals and KangaBio established strategic collaboration to accelerate antibody drug development and innovation

On August 27, 2022 Sanyou Biopharmaceuticals (Shanghai) Co., Ltd. (Sanyou) and Shanghai KangaBio Co., Ltd. (KangaBio) reported that they have reached an antibody drug licensing agreement, regarding a proprietary monoclonal antibody drug developed by Sanyou, which grants KangaBio an exclusive license to exploit the antibody for research, development, manufacturing and commercialization of immunotherapy products (Press release, Sanyou Biopharmaceuticals, AUG 27, 2022, View Source [SID1234618716]). KangaBio, as a rising star biotechnology company, is committed to developing innovative prodrugs and providing innovative medicine to address unmet clinical needs. While Sanyou is a biological high-tech company focusing on innovative antibody drugs R&D services. Based on the two companies’ respective strengths and industry resources, Sanyou and KangaBio will work together to contribute to the development of innovative prodrugs for immunotherapy.

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Previously, KangaBio and Sanyou reached a collaboration agreement on two monoclonal antibody drugs developed by Sanyou and signed high-level term sheet. In addition to the license transfer of drug candidates, the two companies have also successively reached to collaborative development, commissioned R&D, technical services and other forms of staged R&D collaboration. Sanyou fully exploits its 6 types of one-stop innovative antibody drug integrated services, 11 types of flexible and adaptable antibody drug R&D staged technical services and 11 types of diverse antibody generation featured services to fully support the drug development of KangaBio.

Dr. Weidong Jiang, founder and CEO of KangaBio, said, "We are looking forward to this collaboration. KangaBio is committed to developing low toxicity and high efficacy immuno-agonists and innovative prodrugs of multi-specific antibodies. This strategic partnership with Sanyou is expected to utilize the advantages of Sanyou’s internationally leading innovative antibody drug development and value transformation platform, to further enrich KangaBio’s innovative product pipeline, to accelerate the R&D of our innovative antibody drugs and to address unmet clinical needs."

Dr. Guojun Lang, founder and CEO of Sanyou, said, " We are extremely honored to collaborate with KangaBio again. During the past numerous collaborations, Sanyou has saved valuable time with the pre-clinical drug R&D for KangaBio, owing to the comprehensive innovative drug development system and rich industrialization experiences. The close collaboration also demonstrates the strong complementary character of our business layout. We look forward to more in-depth communication and collaboration with KangaBio in the future and wish that this collaboration will bring benefits to the development of KangaBio. Sanyou and Kanga will team up to accomplish remarkable achievements.

Final Analysis of Phase 2 GRIFFIN Study Presented for DARZALEX® (daratumumab)-based Investigational Quadruplet Regimen in Patients with Newly Diagnosed, Transplant-Eligible Multiple Myeloma

On August 27, 2022 The Janssen Pharmaceutical Companies of Johnson & Johnson reported the final results from the randomized Phase 2 GRIFFIN study evaluating the investigational use of DARZALEX (daratumumab) in combination with lenalidomide (Revlimid), bortezomib (VELCADE) and dexamethasone (DARZALEX-RVd), followed by maintenance therapy with DARZALEX-lenalidomide (R), compared to RVd followed by maintenance therapy with R alone, in patients with newly diagnosed, transplant-eligible multiple myeloma (Press release, Johnson & Johnson, AUG 27, 2022, View Source [SID1234618717]). Data were presented in the plenary session at the 19th International Myeloma Society (IMS) Annual Meeting.

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In the primary analysis (median follow-up of 13.5 months), the GRIFFIN study met its primary endpoint, resulting in a higher stringent complete response (sCR) rate for DARZALEX-RVd compared with RVd alone by the end of post-autologous stem cell transplant (ASCT) consolidation therapy (42.4 percent vs. 32 percent; 1-sided P=0.0680) meeting the prespecified 1-sided alpha of 0.1. At IMS, the predefined final analysis for GRIFFIN (median follow-up of 49.6 months), which occurred after all patients had completed at least one year of follow-up after end of study therapy or withdrew, showed that longer progression-free survival (PFS) was observed in patients who received DARZALEX-RVd/DARZALEX-R compared to those who received RVd/R (hazard ratio = 0.45; 95 percent confidence interval, 0.21-0.95; P=0.0324).1 Higher minimal residual disease (MRD) negativity rates were observed for DARZALEX-RVd vs. RVd (64 percent vs. 30 percent). No new safety concerns were observed with longer-term follow-up.

"The final analysis of the GRIFFIN trial highlights the potential benefit of adding daratumumab to RVd for the treatment of newly diagnosed, transplant-eligible patients," said Douglas W. Sborov†, M.D., M.S., Director of the Multiple Myeloma Program at the Huntsman Cancer Institute at the University of Utah and GRIFFIN study investigator. "We are constantly investigating the role of new regimens and combinations to improve outcomes in our patients and GRIFFIN is another important step forward in this research."

Final Analysis from GRIFFIN

After two years of maintenance therapy, the MRD negativity rate continued to favor DARZALEX-RVd versus RVd (64 percent vs. 30 percent; P=<0.0001). Additionally, 44 percent of patients who received DARZALEX-RVd achieved sustained MRD negativity lasting 12 months or more, compared to 14 percent of patients in the RVd arm. Treatment with DARZALEX-RVd also resulted in higher sCR rates at all time points in the study, with the highest rates occurring following two years of maintenance therapy (67 percent vs. 48 percent; P=0.0079, respectively). CR or better rate was 83 percent in the DARZALEX-RVd arm vs. 60 percent in the RVd arm (P=0.005).

At the conclusion of the final analysis, after a median follow-up of 49.6 months, a 55 percent reduction in the risk of disease progression or death was observed in patients in the DARZALEX-RVd arm; an estimated 48-month PFS rate of 87.2 percent was observed in the DARZALEX-RVd arm, compared to 70 percent in the RVd arm. Median PFS was not reached in either treatment arm. In addition, after extended follow-up, no new safety concerns were observed.

"The Phase 2 GRIFFIN study showed important results with the investigational DARZALEX quadruplet regimen in the treatment of newly diagnosed, transplant-eligible multiple myeloma," said Imran Khan, M.D., Ph.D., U.S. Vice President, Medical Affairs, Hematology at Janssen Scientific Affairs, LLC. "The evaluation of this treatment regimen will continue as part of the registrational, Phase 3 PERSEUS study. These studies represent our ongoing focus in multiple myeloma and our commitment to advance research and new therapeutic combinations for patients at each stage of their treatment journey."

About the GRIFFIN Study

The Phase 2 GRIFFIN (NCT02874742) study evaluated the investigational regimen of DARZALEX in combination with RVd and enrolled and treated more than 200 adults ages 18-70 years with newly diagnosed multiple myeloma who were eligible for ASCT.

In the safety run-in cohort, 16 patients received 25 mg of lenalidomide orally on days 1-14; 1.3 mg/m2 of bortezomib subcutaneously on days 1, 4, 8 and 11; and 20 mg of dexamethasone on days 1, 2, 8, 9, 15 and 16, and every 21 days during the induction and consolidation phases (cycles 1-6). DARZALEX 16 mg/kg IV was given on days 1, 8 and 15 of cycles 1-4 and on day 1 of cycles 5-6.

During the maintenance phase (cycles 7-32), patients received 10 mg daily of lenalidomide (15 mg beginning at cycle 10 if tolerated) on days 1-21 every 28 days and DARZALEX 16 mg/kg IV every 56 days; this was amended to every 28 days based upon emerging clinical pharmacokinetic data demonstrating improved target saturation with every-4-week maintenance dosing. Maintenance therapy with lenalidomide could be continued beyond cycle 32, per local standard of care.

In the subsequent randomized Phase 2 portion of the study, 207 patients were randomized to treatment with RVd induction and consolidation, ASCT, and maintenance therapy with lenalidomide; or DARZALEX-RVd, ASCT, and maintenance therapy with DARZALEX and lenalidomide.

Janssen’s clinical development program continues to evaluate the potential of DARZALEX-containing quadruplet regimens in improving clinical outcomes for patients.

About DARZALEX

Janssen is committed to exploring the potential of DARZALEX (daratumumab) for patients with multiple myeloma across the spectrum of the disease. DARZALEX has been approved in eight indications, three of which are in the frontline setting, including newly diagnosed patients who are transplant eligible and ineligible.2

In August 2012, Janssen Biotech, Inc. and Genmab A/S entered a worldwide agreement, which granted Janssen an exclusive license to develop, manufacture and commercialize daratumumab. DARZALEX has become a backbone therapy in the treatment of multiple myeloma, having been used in the treatment of more than 300,000 patients worldwide and more than 68,000 patients in the U.S. alone since its U.S. FDA approval in 2015.3 DARZALEX is the first CD38-directed antibody approved globally to treat multiple myeloma.5

CD38 is a surface protein that is present in high numbers on multiple myeloma cells, regardless of the stage of disease.4 DARZALEX binds to CD38 and inhibits tumor cell growth, causing myeloma cell death.4 DARZALEX may also have an effect on normal cells.4 Data across eight Phase 3 clinical trials, in both the frontline and relapsed settings, have shown that DARZALEX-based regimens resulted in significant improvement in PFS and/or OS.5,6,7,8,9,10,11,12

About Multiple Myeloma

Multiple myeloma is an incurable blood cancer that affects a type of white blood cell called plasma cells, which are found in the bone marrow.2,3 When damaged, these plasma cells rapidly spread and replace normal cells with tumors in the bone marrow. In 2022, it is estimated that more than 34,000 people will be diagnosed and close to 12,000 will die from the disease in the U.S.13 While some patients with multiple myeloma have no symptoms, most patients are diagnosed due to symptoms, which can include bone fracture or pain, low red blood cell counts, tiredness, high calcium levels, kidney problems or infections.4

INDICATIONS

DARZALEX (daratumumab) is indicated for the treatment of adult patients with multiple myeloma:

In combination with lenalidomide and dexamethasone in newly diagnosed patients who are ineligible for autologous stem cell transplant and in patients with relapsed or refractory multiple myeloma who have received at least one prior therapy
In combination with bortezomib, melphalan, and prednisone in newly diagnosed patients who are ineligible for autologous stem cell transplant
In combination with bortezomib, thalidomide, and dexamethasone in newly diagnosed patients who are eligible for autologous stem cell transplant
In combination with bortezomib and dexamethasone in patients who have received at least one prior therapy
In combination with carfilzomib and dexamethasone in patients with relapsed or refractory multiple myeloma who have received one to three prior lines of therapy
In combination with pomalidomide and dexamethasone in patients who have received at least two prior therapies including lenalidomide and a proteasome inhibitor
As monotherapy in patients who have received at least three prior lines of therapy including a proteasome inhibitor (PI) and an immunomodulatory agent or who are double-refractory to a PI and an immunomodulatory agent
IMPORTANT SAFETY INFORMATION

CONTRAINDICATIONS

DARZALEX is contraindicated in patients with a history of severe hypersensitivity (eg, anaphylactic reactions) to daratumumab or any of the components of the formulation.

WARNINGS AND PRECAUTIONS

Infusion-Related Reactions

DARZALEX can cause severe and/or serious infusion-related reactions including anaphylactic reactions. These reactions can be life–threatening, and fatal outcomes have been reported. In clinical trials (monotherapy and combination: N=2066), infusion-related reactions occurred in 37% of patients with the Week 1 (16 mg/kg) infusion, 2% with the Week 2 infusion, and cumulatively 6% with subsequent infusions. Less than 1% of patients had a Grade 3/4 infusion-related reaction at Week 2 or subsequent infusions. The median time to onset was 1.5 hours (range: 0 to 73 hours). Nearly all reactions occurred during infusion or within 4 hours of completing DARZALEX. Severe reactions have occurred, including bronchospasm, hypoxia, dyspnea, hypertension, tachycardia, headache, laryngeal edema, pulmonary edema, and ocular adverse reactions, including choroidal effusion, acute myopia, and acute angle closure glaucoma. Signs and symptoms may include respiratory symptoms, such as nasal congestion, cough, throat irritation, as well as chills, vomiting, and nausea. Less common signs and symptoms were wheezing, allergic rhinitis, pyrexia, chest discomfort, pruritus, hypotension and blurred vision.

When DARZALEX dosing was interrupted in the setting of ASCT (CASSIOPEIA) for a median of 3.75 months (range: 2.4 to 6.9 months), upon re-initiation of DARZALEX, the incidence of infusion-related reactions was 11% for the first infusion following ASCT. Infusion-related reactions occurring at re-initiation of DARZALEX following ASCT were consistent in terms of symptoms and severity (Grade 3 or 4: <1%) with those reported in previous studies at Week 2 or subsequent infusions. In EQUULEUS, patients receiving combination treatment (n=97) were administered the first 16 mg/kg dose at Week 1 split over two days, ie, 8 mg/kg on Day 1 and Day 2, respectively. The incidence of any grade infusion-related reactions was 42%, with 36% of patients experiencing infusion-related reactions on Day 1 of Week 1, 4% on Day 2 of Week 1, and 8% with subsequent infusions.

Pre-medicate patients with antihistamines, antipyretics, and corticosteroids. Frequently monitor patients during the entire infusion. Interrupt DARZALEX infusion for reactions of any severity and institute medical management as needed. Permanently discontinue DARZALEX therapy if an anaphylactic reaction or life-threatening (Grade 4) reaction occurs and institute appropriate emergency care. For patients with Grade 1, 2, or 3 reactions, reduce the infusion rate when re-starting the infusion.

To reduce the risk of delayed infusion-related reactions, administer oral corticosteroids to all patients following DARZALEX infusions. Patients with a history of chronic obstructive pulmonary disease may require additional post-infusion medications to manage respiratory complications. Consider prescribing short- and long-acting bronchodilators and inhaled corticosteroids for patients with chronic obstructive pulmonary disease.

Ocular adverse reactions, including acute myopia and narrowing of the anterior chamber angle due to ciliochoroidal effusions with potential for increased intraocular pressure or glaucoma, have occurred with DARZALEX infusion. If ocular symptoms occur, interrupt DARZALEX infusion and seek immediate ophthalmologic evaluation prior to restarting DARZALEX.

Interference With Serological Testing

Daratumumab binds to CD38 on red blood cells (RBCs) and results in a positive indirect antiglobulin test (indirect Coombs test). Daratumumab-mediated positive indirect antiglobulin test may persist for up to 6 months after the last daratumumab infusion. Daratumumab bound to RBCs masks detection of antibodies to minor antigens in the patient’s serum. The determination of a patient’s ABO and Rh blood type is not impacted. Notify blood transfusion centers of this interference with serological testing and inform blood banks that a patient has received DARZALEX. Type and screen patients prior to starting DARZALEX.

Neutropenia and Thrombocytopenia

DARZALEX may increase neutropenia and thrombocytopenia induced by background therapy. Monitor complete blood cell counts periodically during treatment according to manufacturer’s prescribing information for background therapies. Monitor patients with neutropenia for signs of infection. Consider withholding DARZALEX until recovery of neutrophils or for recovery of platelets.

Interference With Determination of Complete Response

Daratumumab is a human immunoglobulin G (IgG) kappa monoclonal antibody that can be detected on both the serum protein electrophoresis (SPE) and immunofixation (IFE) assays used for the clinical monitoring of endogenous M-protein. This interference can impact the determination of complete response and of disease progression in some patients with IgG kappa myeloma protein.

Embryo-Fetal Toxicity

Based on the mechanism of action, DARZALEX can cause fetal harm when administered to a pregnant woman. DARZALEX may cause depletion of fetal immune cells and decreased bone density. Advise pregnant women of the potential risk to a fetus. Advise females with reproductive potential to use effective contraception during treatment with DARZALEX and for 3 months after the last dose.

The combination of DARZALEX with lenalidomide, pomalidomide, or thalidomide is contraindicated in pregnant women because lenalidomide, pomalidomide, and thalidomide may cause birth defects and death of the unborn child. Refer to the lenalidomide, pomalidomide, or thalidomide prescribing information on use during pregnancy.

ADVERSE REACTIONS

The most frequently reported adverse reactions (incidence ≥20%) were upper respiratory infection, neutropenia, infusion–related reactions, thrombocytopenia, diarrhea, constipation, anemia, peripheral sensory neuropathy, fatigue, peripheral edema, nausea, cough, pyrexia, dyspnea, and asthenia. The most common hematologic laboratory abnormalities (≥40%) with DARZALEX are neutropenia, lymphopenia, thrombocytopenia, leukopenia, and anemia .

InDex Pharmaceuticals Holding AB (publ) interim report January – June 2022

On August 26, 2022 InDex Pharmaceuticals Holding AB (publ) reported that interim report January – June 2022 (Press release, InDex Pharmaceuticals, AUG 26, 2022, View Source [SID1234618701])

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Period April – June 2022
Net sales amounted to SEK 0.0 (0.0) million
Operating loss amounted to SEK –21.7 (–42.6) million
Result after tax amounted to SEK –21.7 (–42.6) million, corresponding to SEK –0.04 per share (–0.08) before and after dilution
Cash flow from operating activities amounted to SEK –53.0 (–45.1) million
Period January – June 2022
Net sales amounted to SEK 0.0 (0.0) million
Operating loss amounted to SEK –40.6 (–51.9) million
Result after tax amounted to SEK –40.6 (–52.0) million, corresponding to SEK –0.08 per share (–0.11) before and after dilution
Cash flow from operating activities amounted to SEK –71.4 (–53.6) million
Cash and cash equivalents at the end of the period amounted to SEK 395.6 (478.8) million
Number of employees at the end of the period was 7 (7)
Number of shares at the end of the period was 532,687,650
All comparative amounts in brackets refer to the outcome during the corresponding period 2021.

Significant events during the quarter
Peter Zerhouni stepped down as CEO of InDex. The company’s CFO Johan Giléus has been appointed acting CEO while a new CEO is being recruited
InDex strengthened the organisation with Eva Arlander as Chief Development Officer and presented a new management team
Significant events after the reporting period
InDex got a new patent for cobitolimod granted in Europe
Other events
InDex participated with a booth at the Digestive Disease Week (DDW) in San Diego
The annual general meeting in InDex Pharmaceuticals Holding AB was held on June 1, 2022
CEO statement
We remain fully focused on the implementation of the phase III study CONCLUDE, which evaluates the drug candidate cobitolimod as a new and unique treatment for patients with moderate to severe left-sided ulcerative colitis. The study is progressing according to plan, i.e. we expect the results to be available during H2 2023. We see great interest in the study and cobitolimod when we, together with our experienced CRO, Parexel Biotech, visit the participating clinics. In the beginning of July, we invited all CRAs of the study, i.e. Parexel’s employees who have ongoing contact with the participating clinics, to a two-day meeting in Stockholm. The purpose of the meeting was to jointly discuss the CONCLUDE study and the benefits of cobitolimod.

At the end of June, the planned consultation meeting with the Japanese regulatory authority, PMDA, was held. It was very encouraging that the PMDA supports our proposed clinical development plan for cobitolimod and that they agree to include Japanese patients in our second induction study in the phase III program, without conducting any specific clinical studies in Japanese subjects. In addition, complementary pharmacokinetic data for cobitolimod in Japanese patients can be collected during the remaining phase III program. This is a unique decision by the PMDA, indicating great potential for cobitolimod and a need for new treatment options that can help more patients with moderate to severe ulcerative colitis. In addition, the positive feedback from PMDA is advantageous for discussions with potential candidates for strategic collaborations in Japan.

At the end of May, InDex participated with a booth at the premier medical congress in the world in gastroenterology, the Digestive Disease Week (DDW) in San Diego, USA. Our participation was very successful and resulted in many valuable contacts, and several new clinics expressed interest to join our phase III study with cobitolimod. We will take the experience with us when we now plan for our participation in the United European Gastroenterology Week (UEGW) in October.

In parallel with the global clinical phase III study CONCLUDE, InDex is conducting a smaller clinical pharmacokinetic study (PK study) with cobitolimod in Sweden. The patient recruitment in the PK study has gone faster than expected and the study is well underway. The aim of the study is to confirm that the systemic uptake of cobitolimod is limited, which has been shown in previous preclinical and clinical studies. The study will include at least 6 patients with moderate to severe ulcerative colitis treated with doses of 500 mg of cobitolimod administered rectally. A limited systemic uptake is a significant advantage compared to competing drugs for ulcerative colitis that act on the whole body and can cause severe side effects outside the inflamed colon.

In July, we announced that a new patent for cobitolimod has been granted in Europe. The patent provides additional protection for the use of cobitolimod in the treatment of inflammatory bowel disease. The patent provides an exclusivity period until August 2040, and further strengthens, broadens and extends our robust intellectual property position for cobitolimod in Europe. Corresponding patent applications have been filed in the strategically most important patent territories globally.

With great interest from the clinics for our phase III study and cobitolimod, our successful interactions with the Japanese regulatory authority, as well as with a strengthened patent portfolio, I look forward to an exciting and eventful fall where we will take important steps forward for InDex.

The full report is attached as a PDF and is available on the company’s website View Source

Publication
This information is information that InDex Pharmaceuticals Holding AB (publ) is obliged to make public pursuant to the EU Market Abuse Regulation (MAR). The information was submitted for publication through the agency of the contact person set out above at 8:00 CET on August 26, 2022.

The NDA for New Indication of Henlius Anti-PD-1 mAb Serplulimab in Combination with Chemotherapy for the First-line Treatment of Patients with Esophageal Squamous Cell Carcinoma Accepted by the NMPA

On August 26, 2022 Shanghai Henlius Biotech, Inc. (2696.HK) reported that the NDA for new indication of HANSIZHUANG, serplulimab, an anti-PD-1 mAb independently developed by the company, in combination with chemotherapy for the first-line treatment of patients with locally advanced/recurrent or metastatic esophageal squamous cell carcinoma (ESCC) has been accepted by the National Medical Products Administration (NMPA) (Press release, Shanghai Henlius Biotech, AUG 26, 2022, View Source [SID1234622747]). HANSIZHUANG has been approved by NMPA for the treatment of microsatellite instability-high (MSI-H) solid tumors, and the NDAs of first-line squamous non-small cell lung cancer (sqNSCLC) and first-line extensive-stage small cell lung cancer (ES-SCLC) indications have been accepted. ESCC is the fourth indication for HANSIZHUANG has been accepted by NMPA.

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Professor Jing Huang, the principal investigator of ASTRUM-007 from Cancer Hospital Chinese Academy of Medical Sciences, said, "ASTRUM-007 is a phase 3 clinical study enrolled locally advanced/recurrent or metastatic ESCC patients with PD-L1 CPS≥1 of serplulimab. In the planned interim analysis evaluated by the Independent Data Monitoring Committee (IDMC), the study has met the co-primary endpoints, providing evidence of safety and efficacy. PD-1 inhibitors combined with chemotherapy has become the first-line standard treatment for advanced esophageal cancer in China. We are hoping that the approval of HANSIZHUANG for the treatment of ESCC comes soon and bring a new treatment option to patients living with ESCC. "

Mr. Jason Zhu, President of Henlius, said, "HANSIZHUANG is an innovative mAb independently developed by Henlius, and ESCC is the fourth indication for which the company filed application. Based on the large number of unmet clinical needs as well as the intractable cancers both globally and in China, we developed differentiation strategy around serplulimab to promote the combination immunotherapy of HANSIZHUANG and clinical research, thereby benefiting more patients in China and around the world."

Esophageal cancer is high incidence in China. According to estimates of the prevalence of malignant tumours in China in 2016, there were 253,000 new cases and 194,000 deaths of esophageal cancer, ranking sixth and fifth in malignant tumors in China, respectively[2]. Since the symptoms of early esophageal cancer are often subtle, most patients are diagnosed in the middle or late stages, missing out on surgical treatment. The mainly treatment for advanced patients is systematic treatment (chemotherapy or targeted therapy), but the treatment result is often limited with the highly recurrence and metastasis rate. Therefore, new drugs and treatments are urgently needed. In recent years, immuno-oncology therapy has become one of the research priorities at home and abroad. Many studies have shown that anti-PD-1 mAb combined with chemotherapy can bring survival benefits to patients with esophageal cancer. Immune checkpoint inhibitor combined with chemotherapy has become the first-line standard treatment for esophageal cancer in China[3].

The NDA is mainly based on the results from a randomized, double-blind, multicenter phase 3 clinical study (ASTRUM-007) comparing HANSIZHUANG in combination with chemotherapy (Cisplatin + 5-FU) or placebo in combination with chemotherapy (Cisplatin + 5-FU) as a first-line treatment for patients with locally advanced/recurrent or metastatic esophageal squamous cell carcinoma. In May 2022, the results of interim analysis conducted by IDMC stated that HANSIZHUANG in combination with chemotherapy showed a significant improvement in PFS and OS against placebo in combination with chemotherapy, which met the pre-defined efficacy criteria, with good safety and no detection of new safety signal.

Underpinned by the patient-centric strategy, serplulimab clinical layout covered high incidence tumours

HANSIZHUANG (serplulimab) is the first innovative mAb developed by Henlius. It has been approved by the NMPA for the treatment of microsatellite instability-high (MSI-H) solid tumours. Henlius actively promotes HANSIZHUANG in conjunction with in-house products of the company such as tumour-specific target, angiogenesis target, immunotherapeutic target, etc. and chemotherapy drugs to conduct immune combination therapies. Underpinned by the patient-centric strategy, Henlius has carried out a differentiated and multi-dimensional layout in the field of gastrointestinal cancer and lung cancer, covering a wide variety of indications, such as lung cancer, hepatocellular carcinoma, ESCC, head and neck squamous cell carcinoma and gastric cancer, etc. Up to date, more than 3,100 subjects have been enrolled worldwide for HANSIZHUANG clinical trials.

In the field of gastrointestinal cancer, HANSIZHUANG has been approved for the treatment of MSI-H solid tumours, which could benefit for patients with MSI-H colorectal cancer and MSI-H gastric cancer. In addition, PD-1 inhibitors are less explored in neoadjuvant/adjuvant therapies for gastric cancer, and Henlius has led the way with a Phase 3 clinical study, striving to benefit gastric cancer patients from the early line of immunotherapy. As for the first-line lung cancer treatment, HANSIZHUANG would potentially be the world’s first PD-1 inhibitor for the first-line treatment of SCLC. Furthermore, HANSIZHUANG was recommended by the 2022 CSCO Guidelines for Diagnosis and Treatment of SCLC for the treatment of ES-SCLC and was also granted orphan drug designation by the FDA for treatment of SCLC.

Going forward, Henlius will continue conducting clinical studies for more innovative products, proactively exploring immuno-oncology combination therapy, bispecific antibodies and the antibody-drug conjugates (ADC), committing to bringing affordable and high-quality innovative biologics to patients around the world.

About Serplulimab

HANSIZHUANG (recombinant humanized anti-PD-1 monoclonal antibody injection, generic name: serplulimab injection) is the first innovative monoclonal antibody developed by Henlius. Up to date, 1 indication is approved for marketing in China, 3 NDAs have been accepted by the NMPA, and 11 clinical trials are ongoing across the world.

HANSIZHUANG was approved by the NMPA for the treatment of MSI-H solid tumors in March 2022 and actively promotes its synergy with in-house products of the company and innovative therapies. It has successively obtained clinical trial licenses in China, the United States, the European Union and other countries and regions to initiate 11 clinical trials on immuno-oncology combination therapies worldwide in a wide variety of indications, such as lung cancer, esophageal carcinoma, head and neck squamous cell carcinoma and gastric cancer, etc., and covering the full range of first-line treatments of lung cancers. As of now, the company has enrolled more than 3,100 subjects in China, Turkey, Poland, Georgia and other countries and regions, and the proportion of Caucasian is over 30% in two MRCTs, making HANSIZHUANG an anti-PD-1 mAb with one of the largest global clinical data pools. The NDAs of the first-line treatment for squamous non-small cell lung cancer (sqNSCLC), extensive small-cell lung cancer (ES-SCLC), and esophageal squamous cell carcinoma (ESCC) have been accepted by the NMPA, which makes HANSIZHUANG potentially the world’s first anti-PD-1 mAb for the first-line treatment of SCLC. Furthermore, HANSIZHUANG was recommended by the 2022 CSCO Guidelines for Diagnosis and Treatment of Small Cell Lung Cancer (SCLC) for the treatment of ES-SCLC and was also granted orphan drug designation by the FDA for treatment of SCLC.

Biomea Fusion Presents Additional Preclinical Data Demonstrating Anti-Tumor Activity and Mechanistic Evidence for BMF-219 in Diffuse Large B-Cell Lymphoma and Multiple Myeloma Models at International Myeloma Society Annual Meeting

On August 26, 2022 Biomea Fusion, Inc. (Nasdaq: BMEA), a clinical-stage biopharmaceutical company dedicated to discovering and developing novel covalent small molecules to treat and improve the lives of patients with genetically defined cancers and metabolic diseases, reported the presentation of two posters at the 19th International Myeloma Society (IMS) Annual Meeting, which took place August 25-27, 2022 in Los Angeles, California (Press release, Biomea Fusion, AUG 26, 2022, View Source [SID1234618704]). Both poster presentations can be viewed on Biomea’s website at View Source

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"Our team has continued to accumulate novel scientific evidence demonstrating compelling preclinical activity of BMF-219 as a potential first-in-class and best-in-class menin inhibitor across a spectrum of tumor types where menin is known to play a critical role. To that end, we are pleased to present additional preclinical data at the IMS Annual Meeting that support the expansion of our ongoing COVALENT-101 clinical trial to enroll patients with DLBCL and MM. We look forward to seeing how BMF-219’s preclinical effect translates to patient benefit in the clinical setting," said Thomas Butler, CEO, Chairman of the Board and Co-Founder of Biomea.

Poster Presentation Details:

Poster P-107: Anti-tumor activity of covalent menin inhibitor, BMF-219, in High-Grade B-Cell Lymphoma and Multiple Myeloma Preclinical Models

Abstract Text:
Introduction

Menin is a scaffold protein that interacts with various transcriptional regulators and partner proteins to promote tumorigenesis in a context-dependent manner. Menin drives oncogenic signaling by regulating expression of genes such as HOXA9 and MEIS1 and is also known to play a key role in MYC-mediated transcriptional activities. BMF-219 is a highly selective, potent, orally bioavailable, small molecule covalent inhibitor of menin. We previously reported the ability of BMF-219 to modulate MYC expression and exhibit high potency against Double HIT Lymphoma (DHL) DLBCL (Diffuse Large B Cell Lymphoma) preclinical models.

Methods
In the current study we demonstrate the anti-tumor activity of BMF-219 in multiple myeloma (MM), and Double/Triple Hit Lymphoma (DHL/THL) and Double Expressor Lymphoma (DEL) high-grade B-cell lymphomas (HGBCL) preclinical models harboring various mutational backgrounds. Additionally, we provide mechanistic evidence for direct inhibition of menin protein, in cell line models representing MM, DHL and DEL.

Results

BMF-219 exhibited high potency in THL and DEL cell lines (IC50 = 0.27 μM and 0.37 μM, respectively), achieving >90% growth inhibition as single agent. BMF-219 was multi-fold more potent and exerted dramatically greater growth inhibition compared to clinical reversible menin inhibitors in all DLBCL cell lines tested, including an expanded panel of DHL cell lines. In ex vivo studies, an R-CHOP refractory THL patient sample and an R-EPOCH refractory MYC-amplified DLBCL patient sample were highly sensitive to BMF-219 treatment (IC50 = 0.15 μM and 0.2 μM, respectively) and demonstrated complete growth inhibition at 1 μM exposure. In contrast, two clinical reversible menin inhibitors demonstrated much lower potency (IC50 = ~1 μM to >10 μM). MM cell lines harboring mutations in TP53, KRAS and NRAS were all sensitive to BMF-219 with growth inhibition IC50 values in the range of 0.25 μM to 0.5 μM and achieved 100% inhibition at 1 μM. Notably, BMF-219 demonstrated single-agent efficacy (IC50 = 0.1 μM to 0.3 μM) against a panel of newly diagnosed and R/R ex vivo MM samples, including a p53-deleted clinical profile. Mechanistically, BMF-219 induced a reduction in menin protein levels, the direct target of this covalent inhibitor. The dose-dependent reduction in menin protein across the collection of MM and DLBCL cell lines with varying cytogenetic and mutational backgrounds will be discussed. Analysis of additional proteins modulated by BMF-219 in these cell line models will also be addressed.

Conclusions:

Collectively, our data demonstrate the novel and robust anti-tumor activity of BMF-219 in HGBCL and MM preclinical models that represent categories of high unmet need. BMF-219 exhibits multi-fold higher potency and complete growth inhibition in these preclinical models compared to clinical reversible menin inhibitors, demonstrating its unique anti-tumor potential in these cancers.

Poster P-269: COVALENT-101: A Phase 1 study of BMF-219, a novel oral covalent menin inhibitor, in patients with relapsed/refractory (R/R) acute leukemia, diffuse large B-cell lymphoma, and multiple myeloma

Abstract Text:
Introduction

Trial in Progress
Background: Menin, a protein involved in transcriptional regulation, impacting cell cycle control, apoptosis, and DNA damage repair, plays a direct role in oncogenic signaling in multiple cancers. Inhibition of menin is a novel approach to cancer treatment. Preclinical data of BMF-219, a highly selective, orally bioavailable, small-molecule covalent inhibitor of menin, show sustained potent abrogation of menin-dependent oncogenic signaling in vitro and in vivo. BMF-219 exhibited a strong anti-proliferative effect on various menin-dependent acute myeloid leukemia (AML) cell lines, diffuse large B-cell lymphoma (DLBCL) lines representing Double/Triple Hit Lymphoma (DHL/THL) & Double Expressor Lymphoma (DEL), and MM cell lines with diverse mutational backgrounds. BMF-219 also showed high potency ex vivo in patient samples from MLL-rearranged and NPM1-mutant AML, THL and MYC-amplified DLBCL, and bone marrow mononuclear cells from treatment-naive and R/R MM.

Methods
COVALENT-101 (BF-MNN-101; NCT05153330) is a prospective, open-label, multi-cohort, non-randomized, multicenter Phase I study evaluating the safety, tolerability, and clinical activity of escalating doses of once daily oral BMF-219 in patients with R/R acute leukemia (AL), DLBCL, and MM who have received or are ineligible for standard therapy. Utilizing an accelerated titration design, doses of BMF-219 will be escalated in single-subject cohorts independently for each indication until 1 subject experiences either a ≥ Grade 2 related adverse event or dose limiting toxicity (DLT). At that point, the cohort will switch to a classical "3 + 3" design. Treatment will continue in 28-day cycles until progression or intolerability. Expansion cohorts for each indication will enroll patients to obtain further safety and efficacy data.

Patients with R/R AL who have failed or are ineligible for any standard therapies, R/R DLBCL following ≥ 2 but ≤ 5 prior therapies, and R/R MM who have received ≥ 3 therapies are eligible. Patients must have ECOG PS ≤ 2, and adequate organ function. Key exclusion criteria include known CNS disease involvement, prior menin inhibitor therapy, and clinically significant cardiovascular disease.

Results
The primary objective is to determine independently for each cohort/indication the optimal biological dose (OBD)/ recommended Phase 2 dose (RP2D) of BMF-219 oral monotherapy. Key secondary objectives include further evaluation of safety and tolerability, characterization of the pharmacodynamics and pharmacokinetics of BMF-219, and assessment of its antitumor activity based on best overall response rate (ORR), duration of response (DOR), progression-free survival (PFS), and time to progression (TTP) per disease specific response criteria as assessed by the investigator. Food-effect studies will be performed in DLBCL and MM patients at certain dose levels.

Conclusions
Enrollment in COVALENT-101 commenced in January 2022.