On November 30, 2021 Treadwell Therapeutics, a clinical stage biotechnology company developing novel therapeutics for highly aggressive cancers, reported that the U.S. Food and Drug Administration (FDA) has approved its Investigational New Drug (IND) application to evaluate CFI-402257, an oral, first-in-class inhibitor of Threonine Tyrosine Kinase (TTK, also as MPS1) in advanced solid tumors and breast cancer (Press release, Treadwell Therapeutics, NOV 30, 2021, View Source [SID1234596246]).

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"TTK is a critical component of the Spindle Assembly Checkpoint and potentially represents a tumor specific vulnerability. Pharmacologic inhibition of TTK using CFI-402257 causes tumor cells to prematurely exit mitosis, leading to increased genomic instability and cell death," said Dr. Mark Bray, Treadwell Chief Scientific Officer and Co-Founder. "CFI-402257 was developed from concept to clinic by our world class team. Preclinical studies and emerging clinical evidence support the use of CFI-402257 in the context of CDK4/6 inhibitor failure in ER+/Her2- breast cancer, a segment where there is a strong unmet need. We are excited by the promise of the molecule in advanced breast cancer and beyond" added Dr. Michael Tusche, Treadwell co-Chief Executive Officer.

Under this IND, Treadwell intends to initiate a Phase 2 clinical trial of CFI-402257 in the first quarter of 2022. This clinical trial is designed to confirm previously efficacious doses and to assess the safety, tolerability, pharmacokinetics, pharmacodynamics and efficacy of CFI-402257 as a single agent in advanced solid tumors, and in combination with fulvestrant in patients with ER+/HER2- advanced breast cancer after disease progression on prior CDK4/6 inhibitor and endocrine therapy. Start-up activities are currently underway.

CFI-402257 is a highly bioavailable, potent and selective inhibitor of TTK. Preclinical studies showed robust inhibition of tumor growth in a wide variety of xenograft models. CFI-402257 also demonstrated durable activity and a manageable safety profile as a single agent and in combination with fulvestrant in advanced ER+ breast cancer in studies conducted at select Canadian sites.

On November 30, 2021 Synaffix B.V., a biotechnology company focused on commercializing its clinical-stage platform technology for the development of antibody-drug conjugates (ADCs) with best-in-class therapeutic index, reported the expansion of its license agreement with Mersana Therapeutics, Inc. (NASDAQ: MRSN), a clinical-stage biopharmaceutical company focused on discovering and developing a pipeline of antibody-drug conjugates (ADCs) targeting cancers in areas of high unmet medical need (Press release, Synaffix, NOV 30, 2021, View Source [SID1234596265]).

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Under the expanded license agreement, Mersana will expand its access to Synaffix’s GlycoConnect site-specific ADC bioconjugation technology for six additional ADC targets. The license rights granted to Mersana are tied to specific ADC targets to be selected and provide non-exclusive access to deploy GlycoConnect site-specific ADC bioconjugation technology against the specified targets. Under the expanded deal, Synaffix is eligible to receive upfront and milestone payments on a per-target basis with a total potential deal value exceeding $1 billion plus royalties. This builds on the long-term relationship between the two companies announced in 2019.

Anna Protopapas, President and Chief Executive Officer of Mersana Therapeutics, said:

"Our collaboration with Synaffix and use of the GlycoConnect site-specific ADC bioconjugation technology has yielded highly innovative ADC products with superior characteristics. Based on the data that we generated to date across multiple programs, we have gained the confidence to significantly expand our collaboration with Synaffix and elect GlycoConnect as our preferred site-specific ADC bioconjugation technology."

Peter van de Sande, Chief Executive Officer of Synaffix, said:

"We are delighted to expand our collaboration with Mersana, a leader in ADC innovation, who will be utilizing our GlycoConnect platform to build out their pipeline with innovative ADC cancer therapeutics. We are honored to see the confidence that Mersana has placed in our platform, demonstrating once again the added value GlycoConnect can bring to innovative ADCs."

Mersana will continue to be responsible for the research, development, manufacturing and commercialization of any resulting ADC products.

This licensing agreement expansion follows three recent ADC technology out-licensing agreements with Kyowa Kirin, a global specialty pharmaceutical company; ProfoundBio, an emerging oncology biotherapeutics company; and Innovent Biologics, a leading biopharmaceutical company developing innovative medicines for the treatment of major diseases. Other collaborators include ADC Therapeutics and Shanghai Miracogen. Twelve ADCs using Synaffix’s technology are currently in development of which three are in clinical development.

On November 30, 2021 NiKang Therapeutics Inc. ("NiKang"), a clinical stage biotech company focused on developing innovative small molecule oncology medicines to help patients with unmet medical needs, reported that it has entered into a clinical trial collaboration and supply agreement with Pfizer Inc. (NYSE: PFE) to evaluate NKT2152, a small molecule that inhibits hypoxia inducible factor 2α (HIF2α), in combination with palbociclib, a CDK4/6 inhibitor, and sasanlimab, a subcutaneously administered PD-1 inhibitor for the treatment of advanced clear cell renal cell carcinoma (ccRCC) (Press release, NiKang Therapeutics, NOV 30, 2021, View Source [SID1234596285]). It will comprise two different combination regimens to treat ccRCC patients who have not responded to or relapsed from prior therapies. Under the terms of the agreement, NiKang will sponsor the study, and Pfizer will co-fund the trials and provide its drugs at no cost to NiKang. The two companies will form a Joint Development Committee to oversee this collaboration.

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"We are excited to work with Pfizer, a company that has been a leader in RCC drug development for nearly two decades, and appreciate its recognition of the potential for these important combination strategies in helping ccRCC patients in need. The scientific rationale of these novel combinations is compelling as they target different and complementary pathways," said Zhenhai Gao, Ph.D., co-founder, president, and CEO of NiKang. "This clinical collaboration provides an excellent framework under which both companies pool their proprietary products and resources together to effectively explore the potential of these combination therapies."

NKT2152 is currently in a phase 1/2 dose escalation and expansion trial (NCT05119335). It is designed to evaluate safety, tolerability, pharmacokinetics, pharmacodynamics and clinical activity in patients with advanced ccRCC. Once an appropriate dose is identified, combination studies including NKT2152 and Pfizer’s palbociclib and sasanlimab will commence.

On November 30, 2021 Jemincare, a leading pharmaceutical company from China, reported its wholly owned subsidiary company, Shanghai Jemincare Pharmaceutical Co., Ltd., had licensed exclusive worldwide ex-China rights to the Kras inhibitor, JMKX1899, to HUYABIO International, the leader in accelerating global development of China’s pharmaceutical innovations (Press release, HUYA Bioscience, NOV 30, 2021, View Source [SID1234596302]). Jemincare will retain the relevant rights in greater China area.

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Kras is one of the most mutated oncogenes in human cancers. The prevalent G12C mutation drives tumor growth and metastasis and has become an important validated target for therapy especially in lung and colorectal cancer. Targeting the GTP pocket of Kras in the switch-II region, which has made Kras druggable, enables the development of more potent and potentially effective inhibitors.

JMKX1899 is a KRAS inhibitor independently developed by Jemincare. Data from preclinical studies shows it has strong blood-brain-barrier crossing capability and has no risk of hERG inhibition and drug-drug-interaction. Jemincare has filed the IND to NMPA in Oct. 2021. The parties will work closely to file IND in US FDA in 2021 to move towards clinical development.

Mr. Hong Liang, President of Jemincare Pharmaceutical Group, said, "We are delighted to work with HUYABIO to explore global development of this unique KRAS inhibitor. This is our first new chemical entity program out-licensed to a global partner. HUYABIO has generated a lot of experience to bring innovative drugs from China to global market. We look forward to generating the clinical efficacy and safety data from global clinical trial since the candidate has huge potential to fill strong unmet needs."

Dr. Mireille Gillings, CEO & Executive Chair of HUYABIO, said, "We are excited to have added the clinical stage Kras inhibitor to our oncology pipeline especially to test in combination with our SHP inhibitor against a variety of solid tumors. We’re delighted to have an excellent partner Jemincare to co-develop combinations that can benefit patients worldwide."

On November 30, 2021 Arcus Biosciences, Inc. (NYSE:RCUS), a clinical-stage, global biopharmaceutical company focused on developing differentiated molecules and combination therapies for people with cancer, and Taiho Pharmaceutical Co., Ltd., ("Taiho"), an R&D driven specialty pharma company with a focus on oncology, reported that Taiho exercised its option for anti-TIGIT antibodies domvanalimab (development code: AB154) and AB308 from Arcus Biosciences ("Arcus"), in Japan and certain other territories in Asia (excluding China) (Press release, Taiho, NOV 30, 2021, View Source [SID1234596229]). This option exercise is based on an option and license agreement between Taiho and Arcus contracted in September 2017. Taiho has already obtained exclusive rights to etrumadenant (AB928), an adenosine A2a/A2b receptor antagonist, and zimberelimab (AB122), an anti-PD-1 monoclonal antibody. This is the third option exercise to an Arcus program.

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In exchange for the exclusive license, Taiho will make an option exercise payment, as well as additional payments upon achievement of clinical, regulatory and commercialization milestones, and, if any products from the program are approved, will pay royalties on net sales of such products.

Domvanalimab is an Fc-silent anti-TIGIT antibody currently under development by Arcus. Similar to PD-1, TIGIT is an immune checkpoint receptor that is expressed on immune cells such as T cells and NK cells. By binding to its ligand CD155, expressed on tumor cells, TIGIT suppresses anti-tumor immune responses, which are thought to be involved with poor prognosis in various types of cancers. Domvanalimab is believed to activate anti-tumor immune responses by blocking CD155 from binding to TIGIT, making it possible for CD155 to bind to and trigger the activating receptor CD226.

Domvanalimab is being developed primarily as a combination therapy with anti-PDx checkpoint inhibitors. The Phase 2 (ARC-7) and Phase 3 (ARC-10) trials of domvanalimab in combination with zimberelimab are currently being conducted by Arcus in first-line metastatic PD-L1≥50% non-small cell lung cancer. A Phase 3 trial (PACIFIC-8) of domvanalimab in combination with durvalumab (Imfinzi, AstraZeneca) is being initiated in Stage III non-small cell lung cancer. Development in other cancer types is also being planned.

Through this collaboration, Taiho will further support the development and commercialization of domvanalimab and will continue its mission to deliver innovative drugs to patients and medical professionals.

About AB308

AB308 is an Fc-enabled anti-TIGIT antibody currently under development by Arcus. In combination with zimberelimab, AB308 is being investigated in an ongoing Phase 1b trial in people with advanced solid and hematologic malignancies.

About Zimberelimab

Zimberelimab is an anti-PD-1 monoclonal antibody currently under development by Arcus. Preliminary data from clinical trials have suggested that zimberelimab has an efficacy and safety profile similar to that of other approved anti-PD-1 monoclonal antibodies.

In addition to combination studies with domvanalimab, Arcus is conducting Phase 1/2 clinical trials of zimberelimab in combination with other Arcus programs in various types of cancers. In Japan, Taiho is conducting a Phase 1 platform trial for zimberelimab in combination with other Taiho products.