On April 12, 2022 Blue Earth Therapeutics, a Bracco company and emerging leader in the development of innovative next generation therapeutic radiopharmaceuticals, reported that the U.S. Food and Drug Administration (FDA) has cleared the Company’s Investigational New Drug Application (IND) application for 177Lu-rhPSMA-10.1 (Press release, Blue Earth Therapeutics, APR 12, 2022, View Source [SID1234612085]). IND authorization to proceed enables Blue Earth Therapeutics to initiate a Phase 1/2 clinical study to evaluate the safety, tolerability, dosimetry and anti-tumor activity of 177Lu-rhPSMA-10.1 in men with metastatic castrate-resistant prostate cancer (mCRPC). 177Lu-rhPSMA-10.1 is the first clinical candidate in Blue Earth Therapeutics’ oncology development program of next generation therapeutic radiopharmaceuticals. Blue Earth Therapeutics holds exclusive worldwide rights to therapeutic applications of radiohybrid Prostate-Specific Membrane Antigen (rhPSMA) radiopharmaceutical technology to help advance the treatment of patients with prostate cancer.

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!

"Clearance to proceed with this first clinical study for 177Lu-rhPSMA-10.1 marks an exciting milestone for our new company, Blue Earth Therapeutics, and the patients with cancer that we hope to serve," said David E. Gauden, D.Phil., Chief Executive Officer of the Company. "We consider 177Lu-rhPSMA-10.1 to be a next generation PSMA therapy with the potential to be best-in-class. 177Lu-rhPSMA-10.1 is the result of a careful optimization process which aimed to maximize therapeutic index by delivering high radiation doses to prostate cancer lesions while sparing normal tissues wherever possible. Excitingly, this optimized technology can be developed with both beta- and alpha-emitting therapeutic radioisotopes. We look forward initially to applying our proven radiopharmaceutical development expertise in advancing 177Lu-rhPSMA-10.1, and, over time, developing a pipeline of additional oncology therapeutics to help address significant unmet patient needs."

The trial is an open-label, multi-center, integrated Phase 1 and 2 study to evaluate the safety, tolerability, radiation dosimetry and anti-tumor activity of 177Lu-rhPSMA-10.1 in men with metastatic castrate-resistant prostate cancer. Phase 1 will investigate the safety, tolerability and dosimetry of multiple cycles of 177Lu-rhPSMA-10.1 in subjects with PSMA-positive mCRPC which has progressed following prior therapy. Results from Phase 1 will be used to determine the recommended treatment regimen to be tested in Phase 2. The Phase 1 study will be conducted at clinical sites in the United States, with further sites added for the Phase 2 component of the trial, in both the United States and Europe.

About Radiohybrid Prostate-Specific Membrane Antigen (rhPSMA)

rhPSMA compounds are referred to as radiohybrid ("rh"), as each molecule possesses three distinct domains. The first consists of a Prostate-Specific Membrane Antigen-targeted receptor ligand which attaches to and is internalized by prostate cancer cells. It is attached to two labelling moieties which may be radiolabeled with either 18F for PET imaging, or with isotopes such as 177Lu or 225Ac for therapeutic use – creating a true theranostic technology. They may play an important role in patient management in the future, and offer the potential for precision medicine for men with prostate cancer. Radiohybrid technology and rhPSMA originated from the Technical University of Munich, Germany. Blue Earth Diagnostics acquired exclusive, worldwide rights to rhPSMA diagnostic imaging technology from Scintomics GmbH in 2018, and therapeutic rights in 2020, and has sublicensed the therapeutic application to its sister company Blue Earth Therapeutics. Blue Earth Therapeutics and Blue Earth Diagnostics work closely on the development of 177Lu-rhPSMA-10.1. Currently, rhPSMA compounds have not received regulatory approval.

On April 12, 2022 Schrödinger, Inc. (Nasdaq: SDGR), whose physics-based software platform is transforming the way therapeutics and materials are discovered, reported that new preclinical data from its Wee1 inhibitor program in a poster session at the American Association of Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting taking place in New Orleans (Press release, Schrodinger, APR 12, 2022, View Source [SID1234612084]). Schrödinger has identified multiple, highly selective and structurally distinct Wee1 inhibitors with optimized physicochemical properties that show strong pharmacodynamic responses and anti-tumor activity in preclinical models. The data presented show that Schrödinger’s Wee1 inhibitors have therapeutic potential for use as monotherapy and as part of combination therapy with other agents.

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 strength of our data underscore the potential of our novel, orally available and potent Wee1 inhibitors and provide an opportunity to advance a potential best-in-class Wee1 inhibitor into the clinic," said Karen Akinsanya, Ph.D., president of R&D, therapeutics, at Schrödinger. "The differentiated and balanced profile of our Wee1 molecules highlights the impact of our computational platform when deployed at scale to overcome design challenges, such as selectivity and ADME optimization. Our unique lead series were identified by assessing more than 445 million potential compounds computationally with only 42 that were synthesized for further analysis."

Wee1 is a gatekeeper checkpoint kinase that prevents cellular progression through the cell cycle, allowing time for DNA repair before cell division takes place. Inhibition of Wee1 allows for accumulation of DNA damage, triggering DNA breakage and apoptosis in tumor cells. Wee1 is emerging as a potentially important therapeutic target for a range of solid tumors, including ovarian and uterine cancer.

Schrödinger is on track to select a Wee1 development candidate later this year. Subject to completion of the preclinical data packages, Schrödinger anticipates submitting an Investigation New Drug (IND) Application to the U.S. Food and Drug Administration (FDA) in 2023.

Additional Details About the Study
The presentation, "Discovery of potent, selective, and orally available Wee1 inhibitors that demonstrate increased DNA damage and mitosis in tumor cells leading to tumor regression in vivo," highlighted preclinical data with multiple lead compounds discovered using Schrödinger’s proprietary physics-based free energy perturbation (FEP+) modeling technology. These molecules demonstrate superior kinase selectivity compared to other known Wee1 inhibitors in a broad kinase panel. In multiple preclinical models, a representative compound, STC-8123, was well tolerated and demonstrated sustained pharmacodynamic and pharmacokinetic properties. The anti-tumor effects of STC-8123 were maintained during dosing holidays while allowing full recovery of mechanism-based hematological effects, likely due to its sustained plasma concentrations and high exposure in tumors. Schrödinger’s advanced Wee1 program compounds maintained potency, selectivity and anti-tumor activity with no detectable time-dependent inhibition of CYP3A4, a key liver enzyme. Taken together, these data support a profile that may enable a favorable dosing regimen and further evaluation of a potential best-in-class Wee1 inhibitor as both monotherapy and as part of combination therapy with other agents.

On April 12, 2022 Osmol Therapeutics, a privately held biopharmaceutical company focused on developing a treatment to prevent chemotherapy-induced peripheral neuropathy (CIPN), reported that it has closed the first $5.2 million tranche of a $7.5 million Series A-1 financing led by Koax Investment Partners, a fund formed by the founders of Biohaven Pharmaceuticals (Press release, Osmol Therapeutics, APR 12, 2022, View Source [SID1234612082]). Osmol’s lead drug candidate, OSM-0205, is based on Dr. Barbara Ehrlich’s research in neuronal calcium sensor-1 (NCS1) and was in-licensed from Yale University. OSM-0205 is designed to prevent the off-target calcium surge caused by taxanes and potentially other chemotherapy treatments associated with peripheral nerve damage.

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 first tranches of our Series A-1 funding announced today will allow Osmol to complete the remaining Investigational New Drug (IND) enabling studies for OSM-0205, our lead drug candidate for the treatment of chemotherapy-induced neuropathy and will allow us to file an IND later this year," said Bob Linke, President and Chief Executive Officer, Osmol Therapeutics. "The remaining capital being raised for the Series A-1 will fund our Phase 1 bioavailability trial in the first half of 2023 and support the initiation of a Phase 2 proof-of-concept clinical study in mid-2023. We believe that OSM-0205 has the potential to address the critical need for a therapy that can prevent CIPN, a condition that can be devastating for cancer patients."

There are currently no Food and Drug Administration (FDA) approved therapies for the prevention or treatment of CIPN, a debilitating condition primarily caused by the off-target toxicity of taxanes and other commonly used chemotherapy treatments.

"Osmol Therapeutics is well-positioned to be a first mover in the treatment of CIPN. We believe that patients deserve a therapy that can reduce or eliminate this debilitating condition," said Robert Berman, M.D., Executive Chairman of Osmol, and Managing Director of Koax Investment Partners. "In addition, Osmol plans to pursue a second indication, chemotherapy induced cognitive impairment, also known as ‘chemobrain.’ OSM-0205 has the potential to provide similar protection to the central nervous system as these chemotherapy treatments cross the blood brain barrier."

About OSM-0205 and CIPN

Osmol’s lead drug, OSM-0205, is based on Dr. Barbara Ehrlich’s research in neuronal calcium sensor-1 (NCS1) at Yale University and is designed to prevent the off-target calcium surge caused by taxanes and potentially other chemotherapy treatments associated with peripheral nerve damage. Data from preclinical studies conducted by Osmol show that pre-treatment with OSM-0205 prevents the pathologic damage caused by these chemotherapy agents. CIPN affects hundreds of thousands of cancer patients every year and can compromise optimal chemotherapy dosing. There are no effective treatments for CIPN, a condition which can diminish quality of life and lead to lifelong disability.

On April 12, 2022 Exai Bio, a next-generation liquid biopsy company, reported data from its scientific research program on the discovery and validation of tumor-specific, orphan non-coding RNAs (oncRNAs), and the validation of artificial intelligence (AI) profiling of oncRNAs to accurately detect cancers of diverse tissue origins (Press release, Exai Bio, APR 12, 2022, View Source [SID1234612080]). With these capabilities, Exai Bio is positioned to develop blood tests for early detection and monitoring of residual disease of many commonly seen cancers.

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!

Exai Bio’s technology is based on its unique, proprietary repertoire of oncRNAs, which are an abundant class of small non-coding RNA sequences that are actively secreted only by cancer cells and not normal tissues. As such, oncRNAs can provide a robust disease signal with high sensitivity, low background and, as a result, high specificity, giving the Exai Bio oncRNA platform several advantages over currently employed mutational or epigenomic analyses of circulating tumor-derived DNA.

In a poster entitled, "Discovery and validation of orphan noncoding RNA profiles across multiple cancers in TCGA and two independent cohorts," Exai Bio is presenting a new study of more than 10,000 samples (7,942 cancer and 3,021 normal samples) from three large independent cancer cohorts. As a first step, Exai Bio identified a large class of distinct oncRNAs that were significantly present in six key cancer types, using samples from The Cancer Genome Atlas (TCGA). These six cancers (breast, colorectal, gastric, kidney, liver, and lung) represent the majority of cancer mortality worldwide.

Next, the oncRNAs from this library were independently validated in two unique IndivuType cohorts, containing 2,245 and 1,252 cancer samples, respectively, and over half of oncRNAs in the library were validated in at least one of the IndivuType cohorts.

Finally, Exai Bio developed artificial intelligence (AI) algorithms in the TCGA cohort for predicting the tissue-of-origin of a cancer sample by analyzing its oncRNA profile. The algorithm was validated and had high accuracy (>91%) in each IndivuType cohort, showing that cancer tissues-of-origin are identifiable based on oncRNA profiles alone.

These results demonstrate that oncRNAs are a unique and generalizable feature of cancers that may be applied to improve the care of cancer patients. Exai Bio is focused on early cancer detection for multiple types of cancer, including the 28 cancer types explored in the TCGA cohort, for which it has identified a proprietary library of more than 250,000 novel oncRNAs. The Exai program aims to build on the current data to translate these findings into a liquid biopsy test with broad utility for early detection of cancer and monitoring of minimal residual disease.

Patrick Arensdorf, Chief Executive Officer, Exai Bio, commented, "We’re proud of the scientific rigor we are applying to the development and validation of an RNA-based liquid biopsy approach for early cancer detection. The evidence reported today demonstrates that Exai Bio’s oncRNA platform is biologically valid, clinically oriented and highly accurate in its ability to predict cancer tissue-of-origin. These results build upon our initial discoveries of tumor-specific oncRNAs in neoadjuvant breast cancer patients and validate the presence of further specific oncRNAs across multiple tumor types. We look forward to translating these findings and advancing the development of our RNA-based liquid biopsy diagnostics platform for early cancer detection and minimal disease monitoring."

Details of the AACR (Free AACR Whitepaper) 2022 poster presentation:
Title: Discovery and validation of orphan noncoding RNA profiles across multiple cancers in TCGA and two independent cohorts
Track: PO.BCS01.05 – Applications of Bioinformatics to Cancer Biology 2
Abstract/Poster: 3353
Authors: Jeffrey Wang, Helen Li, Lisa Fish, Kimberly H. Chau, Patrick Arensdorf, Hani Goodarzi, Babak Alipanahi
Presenter: Jeffrey Wang
Date & Time: April 12, 2022 (1:30 PM – 5:00 PM)
Location: Exhibit Halls, Section 27

Posters will be available on-demand on the AACR (Free AACR Whitepaper) website for attendees (www.aacr.org) beginning at 12:00 PM CDT on April 8, 2022 until July 13, 2022. Upon release at AACR (Free AACR Whitepaper), the poster will be accessible on the publications page of Exai Bio’s website.

On April 12, 2022 Kintara Therapeutics, Inc. (Nasdaq: KTRA) ("Kintara" or the "Company"), a biopharmaceutical company focused on the development of new solid tumor cancer therapies reported that it has entered into definitive agreements with institutional investors for the purchase and sale of 16,226,416 shares of the Company’s common stock (the "Shares") and warrants to purchase 16,226,416 shares of the Company’s common stock (the "Warrants") at a combined purchase price of $0.53 per Share and related Warrant in a registered direct offering priced at-the-market under Nasdaq rules for gross proceeds of approximately $8.6 million, before deducting fees and other offering expenses (Press release, Kintara Therapeutics, APR 12, 2022, View Source [SID1234612076]). The Warrants will have an exercise price of $0.41 per share, will be exercisable immediately and will expire five years from the date of issuance. The closing of the offering is expected to occur on or about April 14, 2022, subject to the satisfaction of customary closing conditions.

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!

A.G.P./Alliance Global Partners is acting as sole placement agent for the offering.

The Company currently intends to use the net proceeds from the offering for funding its clinical studies, working capital and other general corporate purposes, including, but not limited to, funding acquisitions or investments in businesses, products or technologies that are complementary to the Company’s businesses, products and technologies.

The securities described above are being offered by the Company pursuant to a "shelf" registration statement on Form S-3 (File No. 333-254662) filed with the Securities and Exchange Commission (SEC) on March 24, 2021 and declared effective on April 1, 2021. The offering of the securities described herein will be made only by means of a prospectus, including a prospectus supplement, forming a part of the effective registration statement. A final prospectus supplement and accompanying prospectus relating to the securities being offered will be filed with the SEC and will be available on the SEC’s website located at View Source Electronic copies of the prospectus supplement may be obtained, when available, from A.G.P./Alliance Global Partners, 590 Madison Avenue, 28th Floor, New York, NY 10022, or by telephone at (212) 624-2060, or by email at [email protected].

This press release shall not constitute an offer to sell or a solicitation of an offer to buy these securities, nor shall there be any sale of these securities in any state or other jurisdiction in which such offer, solicitation or sale would be unlawful prior to the registration or qualification under the securities laws of any such state or other jurisdiction.