MacroGenics Presents Tebotelimab Data in Patients with Relapsed/Refractory Diffuse Large B-Cell Lymphoma at the 2020 ASH Annual Meeting

On December 7, 2020 MacroGenics, Inc. (NASDAQ: MGNX), a clinical-stage biopharmaceutical company focused on discovering and developing innovative monoclonal antibody-based therapeutics for the treatment of cancer, reported updated results from a dose expansion study of tebotelimab, an investigational, bispecific PD-1 × LAG-3 DART molecule, in patients with diffuse large B-cell lymphoma (DLBCL) (Press release, MacroGenics, DEC 7, 2020, View Source [SID1234572345]). The data were presented at the 62nd Annual Meeting of the American Society of Hematology (ASH) (Free ASH Whitepaper) taking place December 5-8, 2020.

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LAG-3 has been shown to be highly expressed in DLBCL and has emerged as a therapeutic target of interest in this population, while PD-1-targeted therapy has yielded modest efficacy. There remains significant unmet need for patients with relapsed/refractory (R/R) DLBCL.

In one of the tebotelimab monotherapy dose expansion cohorts, 20 DLBCL patients were enrolled, half of whom were CAR T cell therapy experienced. As of the October 23, 2020 data cut-off, there were 13 response-evaluable patients.

A preliminary objective response rate (ORR) of 53.8% (7 of 13 patients) was observed, including responses in five of seven CAR T cell-naïve patients and in two of six CAR T cell experienced patients, the latter of whom both had complete responses. A preliminary duration of response of up to 168 days was observed, with six of seven ongoing responses as of the cut-off date. In the study, baseline LAG-3 expression appeared to associate with clinical response, with additional analyses ongoing.

Tebotelimab was generally well-tolerated among heavily pre-treated R/R DLBCL patients, with manageable infusion-related reactions and no evidence of tumor lysis syndrome. The most common TRAE was pyrexia, which occurred in three (15%) patients. A single Grade 3 TRAE of anemia was observed.

"Although early, the preliminary ORR observed in relapsed/refractory DLBCL patients treated with tebotelimab is promising," said Scott Koenig, M.D., Ph.D., President and Chief Executive Officer of MacroGenics. "Beyond our continued enrollment of patients in the combination study of tebotelimab in solid tumors, we look forward to presenting data from the full cohort of the 20 enrolled DLBCL patients, as well as potentially defining a future registration path for this DART molecule."

About Diffuse Large B-Cell Lymphoma

DLBCL is the most common histologic subtype of non-Hodgkin lymphoma (NHL) accounting for approximately 25 percent of NHL cases globally. According to published research, the incidence in the U.S. and England is approximately 7 cases per 100,000 persons per year, with a median age at presentation of 64 years. DLBCL represents a heterogeneous group of tumors consisting of large, transformed B cells with prominent nucleoli and basophilic cytoplasm, a diffuse growth pattern, and a high proliferation fraction. While DLBCL is curable in approximately half of cases with current therapy, particularly those who achieve a complete remission with first-line treatment, significant unmet medical need remains for patients with relapsed or refractory disease.

About Tebotelimab

Tebotelimab (previously known as MGD013) is an investigational, first-in-class bispecific, tetravalent DART molecule targeting PD-1 and LAG-3. Tebotelimab has been engineered to concomitantly or independently bind to PD-1 and LAG-3 and disrupt these non-redundant inhibitory pathways to further restore exhausted T-cell function. Tebotelimab is being evaluated in a Phase 1 dose expansion study as monotherapy in several tumor types, including both solid tumors and hematological malignancies, and in combination with margetuximab, an investigational Fc-engineered monoclonal antibody targeting HER-2, in three cohorts of patients with advanced HER2-positive cancers (NCT03219268). Tebotelimab will also be evaluated in combination with margetuximab and chemotherapy as part of the ongoing Phase 2/3 MAHOGANY study in patients with HER2-positive gastric or gastroesophageal junction cancer (NCT04082364). MacroGenics’ regional partner in Greater China, Zai Lab, participates in the MAHOGANY study and is also evaluating tebotelimab independently in Phase 1 combination studies with niraparib, a PARP inhibitor, and brivanib, a dual target tyrosine kinase inhibitor of the VEGF and FGF receptors, for the study of advanced gastric cancer and hepatocellular carcinoma, respectively.

Innovent Announces Parsaclisib Treatment Results in High Rate of Rapid and Durable Responses in Patients with Relapsed or Refractory B-Cell Non-Hodgkin Lymphomas

On December 7, 2020 Innovent Biologics, Inc. ("Innovent") (HKEX: 01801), a world-class biopharmaceutical company that develops, manufactures and commercializes high-quality medicines for the treatment of oncology, metabolic, autoimmune and other major diseases, reported data from two ongoing Phase 2 studies evaluating parsaclisib, an Incyte-discovered, potent, highly selective, next-generation oral inhibitor of phosphatidylinositol 3-kinase delta (PI3Kδ), for the treatment of patients with relapsed or refractory follicular (CITADEL-203) and marginal zone (CITADEL-204) lymphomas (Press release, Innovent Biologics, DEC 7, 2020, View Source [SID1234572379]). These data were accepted for presentation at the 62nd American Society of Hematology (ASH) (Free ASH Whitepaper) Annual Meeting and Exposition (ASH 2020), held virtually from December 5–8, 2020.

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The primary endpoint for the CITADEL-203, and -204 studies is objective response rate (ORR); duration of response (DOR), progression-free survival (PFS), overall survival (OS), safety and tolerability are among the secondary endpoints. All radiology-based endpoints are based on independent review committee (IRC) assessment.

Eligible patients received parsaclisib 20 mg once daily for eight weeks followed by either 20 mg once weekly (weekly-dosing group [WG]) or 2.5 mg once daily (daily-dosing group [DG]). Subsequently, daily dosing was selected as the preferred regimen and patients initially enrolled in the WG were allowed to switch to DG. Data are presented for the DG and all patients.

Key results from the CITADEL studies include:

ORR(95%CI), %

mDOR(95%CI),
months

mPFS(95%CI),
months

CITADEL-203: R/R Follicular Lymphoma

DG (N=95)

75(65-83)

14.7(12.0-17.5)

15.8(13.8-19.1)

All (N=118)

73(64-81)

15.9(12.0-NE)

15.8(13.2-19.3)

CITADEL-204: R/R Marginal Zone Lymphoma

DG (N=72)

56.9(44.7-68.6)

NR(8.1-NE)

NR(11.0-NE)

All N=100)

57.0(46.7-66.9)

12.0(9.3-NE)

19.4(13.7-NE)

R/R: relapsed or refractory; ORR: objective response rate; mDOR: median duration
of response (reported for responders); mPFS: median progression-free survival;
DG:daily dosing group.

Parsaclisib was generally well tolerated in all studies with a manageable safety profile.

"We are glad that data from the CITADEL studies presented at ASH (Free ASH Whitepaper) 2020 appear promising, and they highlight the potential of parsaclisib to become a meaningful treatment for patients with relapsed or refractory B-cell non-Hodgkin lymphomas," said Dr. Hui Zhou, Vice President of Oncology Strategy and Medical Sciences of Innovent, "A pivotal Phase 2 registrational trial to evaluate the efficacy and safety of parsaclisib in patients with recurrent and refractory follicular lymphoma or marginal zone lymphoma in China is also recruiting now, and, if successful, the results of this study may help benefit patients with recurrent or refractory indolent B-cell lymphoma and potentially provide more treatment options to the clinicians that treat them."

Presentations are available on the ASH (Free ASH Whitepaper) website at
View Source; #338 (Oral presentation, CITADEL-204), #2935 (Poster, CITADEL-203).

In December 2018, Innovent and Incyte entered into a strategic collaboration for three clinical-stage product candidates, including parsaclisib (PI3Kδ inhibitor). Under the terms of the agreement, Innovent has received the rights to develop and commercialize the parsaclisib and two other assets in Mainland China, Hong Kong, Macau and Taiwan. Currently Innovent is conducting a pivotal Phase 2 registrational trial in China to evaluate the efficacy and safety of parsaclisib in patients with recurrent and refractory follicular lymphoma or marginal zone lymphoma.

About Follicular and Marginal Zone Lymphomas

Follicular lymphoma is a B-cell cancer that originates from the uncontrolled division of specific types of B-cells known as centrocytes and centroblasts. Although it is classified as indolent lymphoma, and the current immunochemotherapy has achieved good efficacy, it still often relapses following by aggressive diseases, which may lead to death within 1 to 2 years. There is an unmet medical need for treatment options for recurrent/refractory follicular lymphoma.

Marginal zone lymphoma is also a group of indolent B-cell lymphoma. Although BTK inhibitors have been approved in the United States to treat recurrent/refractory marginal zone lymphoma, the reported disease free survival after treatment with BTK inhibitors is short, so new treatments need to be developed on the basis of BTK inhibitors.

About Parsaclisib

Parsaclisib is a potent, highly selective, next-generation investigational novel oral inhibitor of phosphatidylinositol 3-kinase delta (PI3Kδ). It is currently under evaluation as a monotherapy in several ongoing Phase 2 trials as a treatment for non-Hodgkin lymphomas (follicular, marginal zone and mantle cell); and autoimmune hemolytic anemia. Pivotal trials of parsaclisib in combination with ruxolitinib for the treatment of patients with myelofibrosis are underway; and there are plans to initiate a trial to evaluate parsaclisib in combination with tafasitamab for B-cell malignancies.

In December 2018, Innovent and Incyte entered into a strategic collaboration for three clinical-stage product candidates, including parsaclisib (PI3Kδ inhibitor). Under the terms of the agreement, Innovent has received the rights to develop and commercialize parsaclisib and two other assets in Mainland China, Hong Kong, Macau and Taiwan.

Through strategic collaboration with genscript probio, initium therapeutics plans to utilize genscript probio’s berkeley lights beacon platform to expand their antibody drug pipeline

On December 7, 2020, GenScript ProBio and Initium Therapeutics reported that Initium Therapeutics has launched a single B-cell based antibody development platform through collaboration with GenScript ProBio (Press release, Initium Therapeutics, DEC 7, 2020, View Source [SID1234629627]). Initium Therapeutics is a US biotechnology company, a spin-off from South Korean biotech company Tiumbio, seeking antibody-based therapeutics for patients who are suffering from unaddressed incurable and rare diseases. The strategic collaboration between the two companies will allow Initium Therapeutics to expand their antibody drug pipeline using GenScript ProBio’s ultra-rapid, high-efficient Berkeley Lights Beacon platform. Furthermore, their partnership will potentially be extended to GenScript ProBio’s cutting edge therapeutic antibody development platforms, including bispecific antibody platform, human antibody transgenic mouse and/or downstream therapeutic antibody development and manufacturing processes. Through this partnership, Initium Therapeutics expects to significantly accelerate their therapeutic antibody pipeline development.

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"We are very pleased to announce that through the strategic collaboration with GenScript ProBio, we will expand our therapeutic antibody pipeline in fibrosis, immuno-oncology and hemophilia," said Dr. Huntaek Kim, CEO of Initium Therapeutics/TiumBio. "Initium Therapeutics was established to develop innovative antibody-based therapeutics focusing on unaddressed rare diseases. Our deep scientific and drug development expertise have allowed us to recognize new therapeutic targets in fibrosis, immuno-oncology and hemophilia, and I believe the partnership with GenScript ProBio will strengthen our therapeutic antibody platform and expand our antibody pipeline in more rapid and highly efficient ways."

"We are very glad to cooperate with Initium Therapeutics and help them expand their therapeutic antibody pipeline in fibrosis, immuno-oncology and hemophilia by utilizing GenScript ProBio’s Berkeley Lights Beacon platform," said Dr. Brian Min, CEO of GenScript ProBio. "Our Single B cell screening platform dramatically expedites and enables unparalleled B cell diversity. We will continue fueling Initium’s first-rate research capabilities and look forward to further collaboration to bring diverse treatment options to patients in rare diseases," he added.

Boehringer Ingelheim Collaborates with Proxygen

On December 7, 2020 Boehringer Ingelheim and Proxygen reported they have entered into a collaboration and license agreement to enable the identification of molecular glue degraders against various oncogenic targets (Press release, Proxygen, DEC 7, 2020, View Source [SID1234574446]). The collaboration combines Proxygen’s unique molecular glue degrader discovery platform and its expertise in targeted protein degradation with Boehringer Ingelheim’s long-term strategy to provide first-in-class, breakthrough therapies for cancer patients.

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Molecular glue degraders and PROTACs harness the power of the cell’s recycling machinery to selectively eliminate disease-causing proteins. Molecular glue degraders achieve this by specifically bridging the distance between target proteins and ubiquitin ligases, which consequently flag the target proteins for rapid degradation. Molecular glues orchestrate this protein-protein proximity through highly cooperative binding. They circumvent the need for a defined binding pocket on the surface of the target protein, a requirement for conventional small molecule drugs, allowing pharmaceutical intervention on proteins that were previously considered undruggable.

"Proxygen’s molecular glue degrader platform has the potential to become a valuable component of Boehringer Ingelheim’s cancer research strategy to treat tumors driven by the most frequently mutated cancer-causing proteins that were previously considered undruggable and to further expand our efforts in the area of targeted protein degradation," says Norbert Kraut, Global Head of Cancer Research at Boehringer Ingelheim. "We are very pleased to partner with Proxygen, complementing our efforts in taking difficult-to-treat cancers on."

The identification of molecular glue degraders has been serendipitous up to this point. Proxygen’s highly scalable and broadly applicable molecular glue discovery platform promises a goal-oriented and comprehensive avenue towards an improved identification of molecular glue degrader candidates.

"We are very excited to join forces with Boehringer Ingelheim," says Bernhard Boidol, Chief Executive Officer of Proxygen. "Working together with a leader in innovative oncological research and development not only validates the broad applicability of our molecular glue degrader platform but also allows us to rapidly develop new therapies for the high unmet medical need of many patients with lung and colorectal cancers."

Proxygen’s new method has recently been recognized by Boehringer Ingelheim through its Grass Roots ‘Innovation Prize’ in Vienna, Austria. The ‘Innovation Prize’ recognizes the innovation power of young life-science companies and bio-entrepreneurs to create and sustain pipelines for the next generation of medicines. Launched in 2015, the Grass Roots programs comprise of ‘Office Hours,’ ‘Academy’ and the ‘Innovation Prize.’ As a company dedicated to improving health and quality of life, these programs give Boehringer Ingelheim the opportunity to lend expertise to the early-stage innovation community and offer guidance around the science to help enable ideas to deliver the next breakthroughs.

Proxygen is entitled to receive up-front payments, research and development support and milestone gated development payments, as well as tiered royalties based on future commercial sales of developed products.

Oncopeptides will host a webcast on Wednesday, December 9[th] at 14:00 (CET) to provide an update regarding data presented at the ASH annual meeting

On December 7, 2020 Oncopeptides AB (publ) (Nasdaq Stockholm: ONCO), a pharmaceutical company focused on the development of targeted therapies for difficult-to-treat hematological diseases reported that the company will host a webcast on Wednesday, December 9th, 2020, at 14:00 (CET) to provide an update regarding the data presented December 4-8 at the American Society Hematology (ASH) (Free ASH Whitepaper) Annual Meeting 2020 (Press release, Oncopeptides, DEC 7, 2020, View Source [SID1234572282]).

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At ASH (Free ASH Whitepaper) Oncopeptides has presented twelve abstracts, including one oral presentation. Key clinical abstracts focused on new data from the ongoing phase 1/2 ANCHOR combination study and new data from the pivotal phase 2 HORIZON study. The preclinical abstracts further explored the mechanism of action of the proprietary peptide-drug conjugate platform in multidrug resistant models of multiple myeloma.

The webcast will be hosted by CEO Marty J Duvall, CSO Jakob Lindberg and CMO Klaas Bakker.

About melflufen
Melflufen (INN melphalan flufenamide) is a first in class peptide-drug conjugate (PDC) that targets aminopeptidases and rapidly releases alkylating agents into tumor cells. Melflufen is rapidly taken up by myeloma cells due to its high lipophilicity and is immediately hydrolyzed by peptidases to release an entrapped hydrophilic alkylator payload. Aminopeptidases are overexpressed in tumor cells and are even more pronounced in advanced cancers and tumors with a high mutational burden. In vitro, melflufen is 50-fold more potent in myeloma cells than the alkylator payload itself due to the increased intracellular alkylator concentration. Melflufen displays cytotoxic activity against myeloma cell lines resistant to other treatments, including alkylators, and has also demonstrated inhibition of DNA repair induction and angiogenesis in preclinical studies. In the pivotal phase 2 HORIZON study melflufen plus dexamethasone demonstrated encouraging efficacy and a clinically manageable safety profile in heavily pretreated patients with relapsed refractory multiple myeloma, with primarily hematologic Adverse Events (AE) and a low incidence of non-hematologic AEs.