On January 4, 2023 Orano Med, a clinical stage radiopharmaceutical company, reported that the first patient has been dosed in a Phase 1 trial of the alpha radioligand therapy with lead-212, 212Pb-GRPR, in patients with advanced solid tumors that express gastrin-releasing peptide receptor (GRPR) (Press release, Orano Med, JAN 4, 2023, View Source [SID1234625852]). 212Pb-GRPR is the first targeted alpha therapy (TAT) targeting GRPR, a protein located on the surface of cells that is highly expressed in prostate cancer, lung cancer, breast cancer and other solid tumors.

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

"Dosing the first patient in our Phase I 212Pb-GRPR clinical trial is a key development milestone for Orano Med in our strategy to develop a pipeline of alpha radiopharmaceuticals targeting difficult to treat cancers," said Julien Dodet, Chief Executive Officer. "The short-range cancer cell killing capabilities of alpha-emitting radioisotopes could mean there is limited toxicity to surrounding healthy cells. Based on promising preclinical results with 212Pb-GRPR, we believe that this first alpha therapy targeting GRPR could significantly improve outcomes for cancer patients who have exhausted other therapies."

212Pb-GRPR is being evaluated in an ongoing, multi-center, single arm, non-randomized, open-label basket trial that will enroll approximately 30 patients with advanced solid tumors. It includes a dose escalation phase followed by an expansion phase. The primary endpoint is to evaluate the safety and tolerability of 212Pb-GRPR. Exploratory efficacy endpoints include objective response rate (ORR), progression-free survival (PFS), and overall survival (OS) using RECIST v1.1 criteria. Additional information about the trial, which is recruiting patients, can be found on clinicaltrials.gov: NCT 05283330.

"We are convinced that targeted alpha therapies, such as 212Pb-GRPR, are the future of radiopharmaceutical therapies, providing an increased cytotoxic potential against cancer cells and the ability to improve treatments in areas of high unmet needs. We were excited about the success of recent beta emitters but believe that alpha radiopharmaceutical therapies will be the next more effective game changer, which will advance the field significantly," said Michael Morris, MD, Founder & Medical Director of Advanced Molecular Imaging and Therapy, the specialist center where the first patient was dosed.

About Targeted Alpha Therapy

Targeted alpha therapy (TAT) relies on a simple concept: combining the ability of biological molecules to target cancer cells with the short-range cell-killing capabilities of alpha-emitting radioisotopes. Alpha decay consists of the emission of a helium nucleus (alpha particle) together with very high linear energy transfer and a range emission of only few cell layers, resulting in irreparable double strand DNA breaks in cells adjacent only to area of alpha emission. This approach results in an increased cytotoxic potential toward cancer cells while limiting toxicity to nearby healthy cells. As a result, alpha emitters are considered as the most powerful payloads to be found for targeted therapies.

About GRPR

Gastrin-releasing peptide receptor (GRPR) is a G-protein-coupled receptor of the family of bombesin receptors. Its ligand, gastrin-releasing peptide (GRP), is a peptide that regulates numerous physiologic functions of the gastrointestinal and central nervous systems, and is overexpressed in a number of cancers, such as prostate, breast, and lung. Oncology research has made tremendous progress in recent years in treatment of these cancers. However, in the 2020’s, around 25,000 patients are expected to be diagnosed with metastatic prostate cancer in the United States, with an average 5-year survival rate of 30%. In breast cancer, around 50,000 patients are expected to have metastatic tumors, with an average 5-year survival rate of 27%.

On January 4, 2023 -SURGE Therapeutics (SURGE) reported that the U.S. Food & Drug Administration (FDA) has accepted its Investigational New Drug (IND) application to proceed with a Phase 1/2a study of its intraoperative immunotherapy, SURGERx with resiquimod (STM-416), for prevention of recurrence and/or progression after transurethral resection of bladder tumor (TURBT) in patients with non-muscle invasive bladder cancer (NMIBC) who were previously diagnosed with high-grade disease and experience recurrence (Press release, SURGE Therapeutics, JAN 4, 2023, View Source [SID1234625851]).

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

"Receiving IND clearance to advance our intraoperative immunotherapy platform into a Phase 1/2a trial in our first indication represents an important milestone as we continue to advance our pipeline," said Michael Goldberg, Ph.D., CEO & Founder of SURGE. "Surgery is presently a physical intervention only, and we believe that it should be a biochemically therapeutic intervention as well. We are excited about the prospects of our novel approach and how it can potentially improve the standard of care for cancer patients in this critical context."

"SURGE’s injectable biodegradable hydrogel enables extended, localized release of various cancer immunotherapies at the site of surgical tumor resection. We look forward to working with Michael and his team at SURGE on this initial Phase 1/2a study to advance their lead intraoperative immunotherapy candidate, STM-416, in patients with recurrent bladder cancer to improve post-resection outcomes," said Seth P. Lerner, M.D., Professor of Urology and holds the Beth and Dave Swalm Chair in Urologic Oncology, in the Scott Department of Urology, Baylor College of Medicine.

SURGE’s proprietary hydrogel has been shown in preclinical studies to reduce post-surgical recurrence and metastasis, which account for 90 percent of cancer-related deaths and have been linked to the immune suppression caused by surgery. Reprogramming the body’s response to surgery from immunosuppressive to immunostimulatory can trigger the patient’s immune system to destroy both local and distal residual cancer cells, reducing recurrence and improving survival.

The SURGERx platform is designed to improve the efficacy and safety of immunotherapy treatment, concentrating the effective dose where and when it can yield tremendous impact. It also potentially increases the number of addressable patients for highly potent molecules that are currently limited to treatment of accessible lesions via intratumoral injection.

On January 4, 2023 TAE Life Sciences (TLS), a biological-targeted radiation therapy company developing next-generation boron neutron capture therapy (BNCT), and AIVITA Biomedical, Inc. (AIVITA), a biotech company specializing in innovative stem cell applications, repoted a partnership to address an unmet need in glioblastoma treatment (Press release, TAE Life Sciences, JAN 4, 2023, View Source [SID1234625850]). Acquiring significant amounts of quality glioblastoma tissue samples has long been a barrier in developing novel cancer therapeutics, with samples often plagued by misleading signals such as dead cells, normal cells and extracellular matrix. The enriched glioblastoma tumor initiating cells (TICs) provided by AIVITA may become targets for novel boron target drugs for future BNCT treatments.

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

"We are thrilled to partner with AIVITA and leverage their ability to identify, isolate and expand high-purity populations of target cell types for therapeutic and diagnostic application," said Bruce Bauer, PhD, CEO of TAE Life Sciences. "This partnership underscores the potential that TAE Life Sciences’ next generation targeted boron drugs and low-energy accelerator-based neutron source holds as a treatment for patients living with the most difficult to treat cancers."

Under the terms of the partnership, AIVITA will provide TICs isolated and expanded from glioblastoma bulk tumors in sufficient quantities as cryopreserved live cell lines to be used by TAE Life Sciences for therapeutic target identification. Among the tumor targets to be identified are cancer biomarkers and biomarkers discovered through genomic analysis that may be novel or unique to an individual patient.

"Advancements in biomarker capture and identification remain an elusive but critical step in improving cancer care," said Hans S. Keirstead, PhD, CEO of AIVITA Biomedical. "I believe this merging of our two leading-edge technologies will lead to meaningful progress in that effort."

On January 4, 2023 RayzeBio, Inc., a targeted radiopharmaceutical company developing an innovative pipeline against validated solid tumor targets, reported that the United States Patent and Trademark Office (USPTO) has issued two patents related to the Company’s lead clinical asset, RYZ101, which uses 225Ac-DOTATATE to treat somatostatin receptor-positive (SSTR+) tumors (Press release, RayzeBio, JAN 4, 2023, View Source [SID1234625849]).

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

The USPTO has issued U.S. Patent No. 11,497,822 and U.S. Patent No. 11,541,134, which are directed to compositions that include 225Ac-DOTATATE and the use of these compositions to treat SSTR+ neuroendocrine tumors, respectively. Both patents are valid until 2042, without taking into account any potential patent term extension.

"RYZ101 is currently being evaluated in two clinical trials and is poised to be the first Ac225 based radiopharmaceutical drug for the industry," said Ken Song, M.D., President and CEO of RayzeBio. "The recognition by the USPTO of our proprietary work with 225Ac-DOTATATE provides us valuable patent protection for the substantive investment we are making to bring forth this medicine to treat cancer patients."

About RYZ101

RYZ101 is an investigational targeted radiopharmaceutical therapy, designed to deliver a highly potent radioisotope, Actinium-225 (Ac225), to tumors expressing the somatostatin receptor type 2 (SSTR2). RYZ101 is being evaluated in clinical studies for patients with SSTR+ gastroenteropancreatic neuroendocrine tumors who have previously been treated with Lu177-based somatostatin therapies and also in patients with extensive stage small cell lung cancer. Details of the study can be found at View Source

On January 4, 2023 Belharra Therapeutics, a privately held drug discovery company with a novel photoaffinity-based, non-covalent chemoproteomics platform, reported a multi-year collaboration with Genentech, a member of the Roche Group (Press release, Belharra Therapeutics, JAN 4, 2023, View Source [SID1234625855]). The companies will collaborate employing Belharra’s proprietary platform to discover and develop small molecule medicines in multiple therapeutic areas including oncology, immuno-oncology, autoimmune, and neurodegenerative diseases.

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

Belharra’s innovative platform builds on a legacy of chemoproteomics drug discovery to identify functional and actionable small molecule ligands for protein targets using a unique approach to capture the interaction of tagged compounds with the human proteome. The company’s proprietary screening library enables Belharra scientists to identify any binding site, on any protein, in any conformational state, in any cell type.

Under the terms of the agreement, Belharra will be responsible for discovery and early preclinical development of small molecules against Genentech’s designated targets, while Genentech will be responsible for late preclinical, clinical, and regulatory development, and commercialization of such small molecules. In return, Belharra will receive an upfront cash payment of $80 million. Over the course of the collaboration, Belharra is eligible to receive development, commercial, and net sales milestones that could exceed $2 billion and a tiered royalty on Genentech’s sale of collaboration products.

For certain oncology or immunology programs to be designated by Genentech, Belharra will have an option to co-develop such programs’ compounds through Phase 1 and to co-fund the remaining development of those programs’ compounds in exchange for a US cost/profit split and ex-US milestone payments and royalties.

"We are excited to work with Genentech and leverage its industry-leading biological acumen to develop novel drug candidates for key therapeutic targets across a range of severe diseases for which patients currently lack adequate treatments," said Jeff Jonker, CEO of Belharra. "Genentech is long recognized for its dedicated pursuit of groundbreaking science to illuminate the drivers of disease and enable the discovery and development of transformational medicines. This collaboration further underscores the promise of Belharra’s novel platform to advance that cause."

"Our collaboration with Belharra gives Genentech access to a drug invention platform that allows us to interrogate important therapeutic pathways and targets that we strongly believe drive disease pathogenesis, but have proven to be inaccessible to conventional approaches," said James Sabry, MD, PhD, Global Head of Pharma Partnering at Roche. "Partnering with early-stage companies like Belharra provides Genentech with yet another way to advance groundbreaking science to discover and develop medicines for patients with serious and life-threatening diseases."