Conformation-X Therapeutics Bolts out of Stealth, Securing Over $13.5M in Funding to Propel Its Innovative Immune-Oncology Pipeline

On April 3, 2024 Conformation-X Therapeutics, LLC, an immune-oncology focused drug development company, reported that it has closed an oversubscribed funding tranche of $3.65M, bringing the total raised since inception to over $13.5M (Press release, Conformation-X Therapeutics, APR 3, 2024, View Source [SID1234641761]). The company unveiled its lead assets by disclosing successful ex vivo and in vivo proof-of-concept studies for its HHLA2 and IL18BP programs, marking critical milestones in the cancer drug development process.

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!

Drawing inspiration from the fundamental role of protein conformations in disease biology and drug efficacy, Conformation-X applies unparalleled precision to developing novel immune checkpoint inhibitors. The company is creating a comprehensive portfolio of differentiated therapeutics addressing cancer mechanisms that have eluded existing treatments.

"The limitations of current checkpoint therapies are evident, as they don’t fully target the diverse spectrum of mechanisms associated with non-responsiveness and treatment resistance," said Dr. Ali H. Munawar, CEO of Conformation-X Therapeutics.

Despite the pivotal role of PD-1/PD-L1 inhibitors in cancer immunotherapy, several peer-reviewed clinical studies have shown that the overall response rate across various cancers remains at or below 20%. Patients facing resistance to conventional checkpoint therapies encounter a range of challenges. This includes tumors that inherently possess low immunogenicity, are less likely to trigger an immune response, and immune exclusion, which restricts immune cells from the tumor microenvironment (TME). Moreover, complex genetic landscapes featuring oncogenic drivers and epigenetic modifications further contribute to immune evasion and influence treatment outcomes.

Dr. Munawar added, "We are committed to pioneering alternative therapeutic options for these patients by targeting novel biology and molecular pathways. The successive rounds of funding are a testament to our investors’ confidence in the innovation and rigor behind our efforts."

The recent capital infusion accelerates the company towards translational studies of its lead asset and facilitates the expansion of its pipeline. The company’s pipeline encompasses diverse drug target classes, extending beyond the current landscape of immune checkpoints to include novel soluble and epigenetic checkpoints while continuing to innovate within the B7-family of receptors.

"Achieving selective therapeutic targeting of HHLA2 demonstrates our team’s profound understanding of its intricate structure-function relationship and the critical role that HHLA2 plays in tumor immune evasion. Our work highlights the strength of Conformation-X’s drug discovery platform," said Dr. Stephen Weeks, Sr. Director of Structural Biology and Biophysics.

TransCode Therapeutics Reports 2023 Results; Provides Business Update

On April 3, 2024 TransCode Therapeutics, Inc. (NASDAQ: RNAZ), the RNA oncology company committed to more effectively treating cancer using RNA therapeutics, reported financial results for 2023 and recent business progress (Press release, TransCode Therapeutics, APR 3, 2024, View Source [SID1234641817]).

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 believe 2023 was extremely productive and pivotal for TransCode. We are proud to have advanced our lead therapeutic candidate, TTX-MC138, into the clinic as a first-in-class drug candidate against metastatic cancer. The year was highlighted by preliminary clinical results from our Phase 0 clinical trial with radiolabeled TTX-MC138," said Tom Fitzgerald, interim CEO and CFO of TransCode. "Further, despite very challenging financial markets, we raised over $25 million in equity financings, streamlined our operations for higher efficiency, and signed two strategic collaborations aimed at demonstrating the value of our TTX platform in additional applications. We also continued to achieve other important milestones, with the ultimate objective of fulfilling the promise of RNA therapeutics for oncology applications. We now look forward to our Phase 1 clinical trial of TTX-MC138 which, subject to FDA authorization, is planned to begin in mid-2024."

Key Highlights (2023 and Q1 2024)

· IRB approval for FDA-cleared first-in-human Phase 0 clinical trial with TTX-MC138.
· First patient dosed and preliminary clinical results with radiolabeled TTX-MC138 in the Phase 0 clinical trial.
· Signed a co-research agreement with Debiopharm to develop nucleic acid therapeutics for cancer treatment.
· Signed a joint research and development agreement with Akribion Genomics to develop a CRISPR-derived technology platform for cancer treatment.
· Raised over $25 million in equity financings in an extremely challenging financial environment.
· Refocused our development strategy, prioritizing advancing TTX-MC138 into a Phase 1 clinical trial and reducing cash burn.
· Appointed CFO Tom Fitzgerald as interim CEO and director Philippe Calais as Executive Chairman following the resignation of Michael Dudley as CEO.
· Appointed Daniel Vlock, M.D., as Chief Medical Officer (part-time).
· Regained compliance with Nasdaq’s stockholders’ equity requirement.
· Presented TransCode technology at leading cancer conferences including San Antonio Breast Cancer Symposium, AACR (Free AACR Whitepaper), OTS, and TIDES Europe.

TTX-MC138

· Reported preliminary clinical results suggesting delivery of TTX-MC138 to metastatic lesions in a patient with breast cancer metastatic to lungs, bone, and liver.
· Reported positive preclinical results in a model of glioblastoma showing successful delivery and pharmacodynamic activity in brain tumors.
· Reported positive preclinical results in a model of metastatic pancreatic adenocarcinoma showing 50% inhibition of metastatic progression compared to standard-of-care chemotherapy.
· Received second Orphan Drug Designation from FDA, for TTX-MC138 in pancreatic cancer.

TTX-siPDL1

· Reported positive preclinical results in pancreatic cancer, showing extended survival relative to standard-of-care chemotherapy.

TTX-RIGA

· Reported successful completion of animal studies in a model of melanoma showing arrest of secondary tumor progression.

2024 Corporate and R&D Objectives

With what we expect will be a very exciting year ahead, our 2024 corporate goals, none of which are assured, are to strengthen our organization while raising sufficient capital to continue to advance our research. We will also seek to expand collaborations with strategic partners to further enhance the value of our pipeline.

2024 will also be a critical year for the clinical development of TTX-MC138 and our preclinical portfolio, as we seek to:

· Initiate a Phase 1 clinical trial with TTX-MC138 in patients with advanced solid tumors as soon as we obtain FDA authorization and relevant institutional review board approvals from investigational sites.
· Report preliminary results from the planned Phase 1 trial later this year.
· Publish preclinical results in the second half of the year supporting TTX-MC138 in glioblastoma and pancreatic cancer, TTX-siPDL1 in pancreatic cancer, and TTX-RIGA in melanoma.
· Continue preclinical studies for therapeutic candidates TTX-mRNA and TTX-CRISPR.
· Advance existing strategic partnerships and sign others around TransCode’s TTX delivery platform, TTX-CRISPR, TTX-siRNA, TTX-MC138, and TTX-mRNA candidates.
· Further develop an exploratory test for miRNA-10b.
· If capital resources permit, initiate CMC development to support future IND-enabling studies with TTX-siPDL1 or TTX-RIGA candidates.

2023 Financial Highlights (amounts are approximate)

· Cash was $2.8 million on December 31, 2023, compared to $4.97 million on December 31, 2022.
· Research and development expenses were $12.3 million in 2023 compared to $10.2 million in 2022.
· General and administrative expenses were $7.2 million in 2023 compared to $8.4 million in 2022.
· Operating loss was $19.4 million in 2023 compared to $18.6 million in 2022.

Financial Guidance

TransCode expects that its cash of approximately $2.8 million as of December 31, 2023, together with approximately $6.2 million in net proceeds received from the sale of common stock and warrants in a January 2024 registered direct offering, will be sufficient to fund planned operations into late third quarter or early fourth quarter of 2024.

Vopec Pharmaceuticals and Agastiya Biotech Announce Breakthrough Phase 1 Study Results of Small Molecule AB001 for Multiple Metastatic Solid Tumors

On April 3, 2024 Vopec Pharmaceuticals and Agastiya Biotech reported topline results from the Phase 1 study of AB001, an investigational small molecule, PDL1 immunotherapy for patients with metastasized and locally advanced solid tumors (Press release, Agastiya Biotech, APR 3, 2024, View Source [SID1234641730]).

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!

Unlike current standard of care immuno- and chemotherapy drugs AB001’s novel immunotherapy mechanism of action selectively destroys tumors without harming healthy cells.

Study Design

A total of 33 patients [3+3 Design], 7 with breast cancer, 5 with ovarian cancer, and 21 with other solid tumors, received AB001. AB001 was administered orally twice daily (at BID doses ranging from 40 to 800 mg) in patients with advanced or metastatic solid tumors. The study’s primary and secondary objectives were safety and efficacy. Safety parameters include MTD, PK, and other standardized toxicology protocols. The efficacy study included investigator-evaluated anti-tumor activity (PD) and biomarker responses correlated with pre- and post-treatment PET-CT and mRNA expression studies.

Toxicity Study

The Phase 1 study showed that AB001 was well-tolerated. The adverse events (AEs) were mild to moderate in severity. No dose-limiting toxic (DLT) effects or treatment-related deaths were reported. Treatment-related adverse events occurred in 9 patients at an instance rate of 2.9%; the most common adverse events were 5 patients with diarrhea (1%), 3 patients with vomiting (1%), and 1 patient with fatigue. Six adverse events were graded as mild in severity, and 3 adverse events were found to be moderate in severity. On investigation, the AEs were determined to be of unrelated causes to the treatment drug and resolved with medications, including over-the-counter medicines.

Efficacy Study

AB001 met secondary efficacy endpoints and demonstrated clinical benefit. The 14-day dose escalation studies showed notable improvements at all dosages in tumor biomarkers, immune markers, and tumor size, as confirmed by 21-day PET SCANs. Among patients with solid tumors, a favorable response was observed in 63.64%, a stable response in 19.39%, and disease progression in 16.36%. Partial responses (PR) were also observed in patients with other solid tumors. Serial assessment of tumor biomarkers showed a significant reduction from baseline. CA19.9 showed a 42% reduction (p=0.2), compared to a 38.4% drop in the CA125 markers (p=0.9), and the overall CEA markers revealed a reduction of 58.6% (p=0.6). mRNA studies showed significant changes in the expression of immunomodulation genes and Treg genes, which were associated with the anti-tumor response of AB001.

The superfast treatment impact within 21 days is attributed to the femto-scale metabolism and tumor DNA damage. MiRNA ad mRNA degradation add to the efficacy of the drug.

AB001 is the first Anti-cancer molecule to be released in India by Vopec Pharmaceutical with R&D and clinical collaboration with US-based Agastiya Biotech. Phase 2 is anticipated to begin in May 2024 in India.

The US FDA has awarded Orphan Drug Designation for AB001 for pancreatic, glioblastoma multiforme (GBM), and acute myeloid leukemia (AML) cancer indications. The companies will present the AB001 Phase 1 data at a future scientific forum.

Soligenix Announces Agreement on the Design of a Second Confirmatory Placebo-Controlled Trial for HyBryte™ With the European Medicines Agency

On April 3, 2024 Soligenix, Inc. (Nasdaq: SNGX) (Soligenix or the Company), a late-stage biopharmaceutical company focused on developing and commercializing products to treat rare diseases where there is an unmet medical need, reported that it has received agreement from the European Medicines Agency (EMA) on the key design components of a confirmatory Phase 3 placebo-controlled study evaluating the safety and efficacy of HyBryte (synthetic hypericin) in the treatment of cutaneous T-cell lymphoma (CTCL) patients with early-stage disease (Press release, Soligenix, APR 3, 2024, View Source [SID1234641746]). This confirmatory 18-week study is expected to enroll approximately 80 patients in the United States and Europe and is targeted to begin patient enrollment by the end of 2024 with top-line results anticipated in the second half of 2026.

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 confirmatory study, called FLASH2 (Fluorescent Light Activated Synthetic Hypericin 2), replicates the double-blind, placebo-controlled design used in the first successful Phase 3 FLASH study that consisted of three 6-week treatment cycles (18 weeks total), with the primary efficacy assessment occurring at the end of the initial 6 week double-blind, placebo-controlled treatment cycle (Cycle 1). However, the second study extends the double-blind, placebo-controlled assessment to 18 weeks of continuous treatment (no "between-Cycle" treatment breaks) with the primary endpoint assessment occurring at the end of the 18-week timepoint. In the first Phase 3 study, a treatment response of 49% (p<0.0001 vs patients receiving placebo in Cycle 1) was observed in patients completing 18 weeks (3 cycles) of therapy. In this second study, all important clinical study design components remain the same as in the first FLASH study, including the primary endpoint and key inclusion-exclusion criteria. The extended treatment for a continuous 18 weeks in a single cycle is expected to statistically demonstrate HyBryte’s increased effect over a more prolonged, "real world" treatment course.

"In treating CTCL, which is a chronic cancer with no cure, long-term safety is a strong driver of treatment choice. Most current treatment options for CTCL are associated with significant safety concerns, including black-box warnings," stated Brian Poligone, MD, PhD, Director of the Rochester Skin Lymphoma Medical Group, Fairport, NY. "Clinical studies with HyBryte have demonstrated strong and rapid efficacy with a very benign safety profile, with broad applicability across different lesion types, different skin tones and different disease stages. I know I can speak for my colleagues that have been involved with these studies when I say that the data generated to date has been extremely compelling. This second study is very similar to the first FLASH study, and should build on these compelling data, while allowing us to more closely treat as we would in a ‘real world’ setting. We believe the outcome of this trial will further validate the utility of HyBryte in early-stage CTCL and we look forward to participating in this important study."

"With its chronic course and major impact on patient quality of life, CTCL is an orphan disease in urgent need of additional treatment options that are well-tolerated and safe over the long term," stated Christopher Schaber, PhD, President and Chief Executive Officer of Soligenix. "Studies to date have indicated a substantial increase in efficacy with longer treatment and similar performance against both patch and plaque lesions. These results are derived from one of the largest studies ever conducted in CTCL, and we believe this second study will both substantiate and improve upon these results. Given our extensive engagement with the CTCL community, our esteemed Medical Advisory Board and our previous trial experience with this disease, we anticipate being able to accelerate enrollment in support of this study, including the potential to enroll previously identified and treated HyBryte patients from the FLASH study. Discussions with the FDA on an appropriate study design remain ongoing. While collaborative, the agency has expressed a preference for a longer duration comparative study over a placebo-controlled trial. Given the shorter time to potential commercial revenue and the similar trial design to the first FLASH study afforded by the EMA accepted protocol, we will initiate that study. At the same time, we will continue discussions with the FDA on modifying the development path to adequately address their feedback."

The confirmatory Phase 3, randomized, double-blind, placebo-controlled, multicenter study includes approximately 80 subjects with early-stage CTCL. It will evaluate the efficacy and safety of HyBryte topically applied to CTCL lesions twice weekly for 18 weeks, with each application followed 21 (±3) hours later by the administration of safe, visible light at a wavelength of 500 to 650 nm. The light will be administered starting at 6 J/cm2 twice weekly. This will be increased upwards by 2 J/cm2 until: 1) the patient experiences a Grade 1 erythema, 2) the patient reaches the maximum dose of 30 J/cm2, or 3) the patient cannot tolerate the treatment time, whichever comes first. All of the patient’s lesions that are readily available for exposure to the visible light source will be treated and 3 to 5 index lesions in each patient will be prospectively identified and indexed for the modified composite assessment of index lesions severity (mCAILS) evaluation prior to randomization (baseline). The primary efficacy endpoint will be assessed on the percent of patients in each of the two treatment groups (i.e., HyBryte and placebo) achieving a Partial or Complete Response (yes/no) of the treated lesions defined as a ≥ 50% reduction in the total mCAILS score for the 3-5 index lesions following 18 weeks of treatment compared to the total mCAILS score at baseline. Other secondary measures will assess treatment response (including duration), degree of improvement, time to relapse and safety. Following treatment, all patients will be followed every 4 weeks for a total of 12 weeks (through Week 30). The Data Monitoring Committee (DMC) will conduct one (1) interim analysis when approximately 60% of the total subjects have completed the primary endpoint evaluation. The primary efficacy endpoint and the key safety endpoints will be analyzed. A sample size recalculation may be performed after examining the assumptions or the trial halted for either futility, safety concerns, or overwhelming efficacy. Soligenix, participating clinical investigators, and any personnel involved in trial conduct will remain blinded to study treatment until completion of the trial.

About HyBryte

HyBryte (research name SGX301) is a novel, first-in-class, photodynamic therapy utilizing safe, visible light for activation. The active ingredient in HyBryte is synthetic hypericin, a potent photosensitizer that is topically applied to skin lesions that is taken up by the malignant T-cells, and then activated by safe, visible light approximately 24 hours later. The use of visible light in the red-yellow spectrum has the advantage of penetrating more deeply into the skin (much more so than ultraviolet light) and therefore potentially treating deeper skin disease and thicker plaques and lesions. This treatment approach avoids the risk of secondary malignancies (including melanoma) inherent with the frequently employed DNA-damaging drugs and other phototherapy that are dependent on ultraviolet exposure. Combined with photoactivation, hypericin has demonstrated significant anti-proliferative effects on activated normal human lymphoid cells and inhibited growth of malignant T-cells isolated from CTCL patients. In a published Phase 2 clinical study in CTCL, patients experienced a statistically significant (p=0.04) improvement with topical hypericin treatment whereas the placebo was ineffective. HyBryte has received orphan drug and fast track designations from the FDA, as well as orphan designation from the EMA.

The published Phase 3 FLASH trial enrolled a total of 169 patients (166 evaluable) with Stage IA, IB or IIA CTCL. The trial consisted of three treatment cycles. Treatments were administered twice weekly for the first 6 weeks and treatment response was determined at the end of the 8th week of each cycle. In the first double-blind treatment cycle (Cycle 1), 116 patients received HyBryte treatment (0.25% synthetic hypericin) and 50 received placebo treatment of their index lesions. A total of 16% of the patients receiving HyBryte achieved at least a 50% reduction in their lesions (graded using a standard measurement of dermatologic lesions, the CAILS score) compared to only 4% of patients in the placebo group at 8 weeks (p=0.04) during the first treatment cycle (primary endpoint). HyBryte treatment in this cycle was safe and well tolerated.

In the second open-label treatment cycle (Cycle 2), all patients received HyBryte treatment of their index lesions. Evaluation of 155 patients in this cycle (110 receiving 12 weeks of HyBryte treatment and 45 receiving 6 weeks of placebo treatment followed by 6 weeks of HyBryte treatment), demonstrated that the response rate among the 12-week treatment group was 40% (p<0.0001 vs the placebo treatment rate in Cycle 1). Comparison of the 12-week and 6-week treatment groups also revealed a statistically significant improvement (p<0.0001) between the two groups, indicating that continued treatment results in better outcomes. HyBryte continued to be safe and well tolerated. Additional analyses also indicated that HyBryte is equally effective in treating both plaque (response 42%, p<0.0001 relative to placebo treatment in Cycle 1) and patch (response 37%, p=0.0009 relative to placebo treatment in Cycle 1) lesions of CTCL, a particularly relevant finding given the historical difficulty in treating plaque lesions in particular.

The third (optional) treatment cycle (Cycle 3) was focused on safety and all patients could elect to receive HyBryte treatment of all their lesions. Of note, 66% of patients elected to continue with this optional compassionate use / safety cycle of the study. Of the subset of patients that received HyBryte throughout all 3 cycles of treatment, 49% of them demonstrated a positive treatment response (p<0.0001 vs patients receiving placebo in Cycle 1). Moreover, in a subset of patients evaluated in this cycle, it was demonstrated that HyBryte is not systemically available, consistent with the general safety of this topical product observed to date. At the end of Cycle 3, HyBryte continued to be well tolerated despite extended and increased use of the product to treat multiple lesions.

Overall safety of HyBryte is a critical attribute of this treatment and was monitored throughout the three treatment cycles (Cycles 1, 2 and 3) and the 6-month follow-up period. HyBryte’s mechanism of action is not associated with DNA damage, making it a safer alternative than currently available therapies, all of which are associated with significant and sometimes fatal, side effects. Predominantly these include the risk of melanoma and other malignancies, as well as the risk of significant skin damage and premature skin aging. Currently available treatments are only approved in the context of previous treatment failure with other modalities and there is no approved front-line therapy available. Within this landscape, treatment of CTCL is strongly motivated by the safety risk of each product. HyBryte potentially represents the safest available efficacious treatment for CTCL. With very limited systemic absorption, a compound that is not mutagenic and a light source that is not carcinogenic, there is no evidence to date of any potential safety issues.

The Phase 3 FLASH study was partially funded by the National Cancer Institute via a Phase II SBIR grant (#1R44CA210848-01A1) awarded to Soligenix, Inc. In addition, the FDA awarded an Orphan Products Development grant to support the evaluation of HyBryte for expanded treatment in patients with early-stage CTCL, including in the home use setting. The grant, totaling $2.6 million over 4 years, was awarded to the University of Pennsylvania that was a leading enroller in the Phase 3 FLASH study.

About Cutaneous T-Cell Lymphoma (CTCL)

CTCL is a class of non-Hodgkin’s lymphoma (NHL), a type of cancer of the white blood cells that are an integral part of the immune system. Unlike most NHLs which generally involve B-cell lymphocytes (involved in producing antibodies), CTCL is caused by an expansion of malignant T-cell lymphocytes (involved in cell-mediated immunity) normally programmed to migrate to the skin. These malignant cells migrate to the skin where they form various lesions, typically beginning as patches and may progress to raised plaques and tumors. Mortality is related to the stage of CTCL, with median survival generally ranging from about 12 years in the early stages to only 2.5 years when the disease has advanced. There is currently no cure for CTCL. Typically, CTCL lesions are treated and regress but usually return either in the same part of the body or in new areas.

CTCL constitutes a rare group of NHLs, occurring in about 4% of the more than 1.2 million individuals living with the disease. It is estimated, based upon review of historic published studies and reports and an interpolation of data on the incidence of CTCL that it affects approximately 30,000 individuals in the U.S. (based on SEER data, with approximately 3,200 new cases seen annually) and over 20,000 individuals in Europe (based on 5-year prevalence data, with approximately 5,600 new cases annually).

Astex Pharmaceuticals Announce Key Data Presentations at the American Association For Cancer Research (AACR) 2024 Annual Meeting

On April 3, 2024 Astex Pharmaceuticals, a pharmaceutical company based in Cambridge, UK, dedicated to the discovery and development of novel small molecule therapeutics for oncology and diseases of the central nervous system, reported that it will make five key data presentations at AACR (Free AACR Whitepaper) 2024 focusing on its Phase II-ready MDM2 antagonist, ASTX295 (Press release, Astex Pharmaceuticals, APR 3, 2024, View Source [SID1234641731]). AACR (Free AACR Whitepaper) 2024 will take place from April 5-10, 2024, at the San Diego Convention Center, San Diego, USA.

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!

ASTX295 data presentations at AACR (Free AACR Whitepaper) 2024

Title Presentation Date/Time/Presenter Link to Abstract
Discovery of ASTX295, a potent, next-generation small molecule antagonist of MDM2 with differentiated pharmacokinetic profile. From concept to clinic Oral Tuesday, April 9
3:20 – 3:35pm PT

Session Title: Novel Antitumor Agents 5

Presenter: Maria Ahn, Astex Pharmaceuticals, UK

6588
View Source!/20272/presentation/4100
ASTX295 engages p53-mediated apoptosis and an inflammatory response in patient derived mesothelioma explants Poster Sunday, April 7
1:30 – 5:00pm PT

Presenter: Dean Fennell, University of Leicester, UK

666
linkView Source!/20272/presentation/4103
Identification of biomarkers of response to MDM2 inhibition in solid tumours using computational, multi-omics approaches

Poster Sunday, April 7
1:30 – 5:00pm PT

Presenter: Matthew Davis, Astex Pharmaceuticals, UK

667
View Source!/20272/presentation/4104
Phase 1 study of MDM2 antagonist ASTX295 in patients with solid tumors with wild-type TP53 Poster Monday, April 8, 9:00 -12:30pm PT
Presenter: Ekaterina Dumbrava, The University of Texas MD Anderson Cancer Center, Houston, TX

CT066
View Source!/20272/presentation/11530
Targeting the MDM2-p53 interaction: Time-and concentration-dependent studies in tumor and normal human bone marrow cells reveal strategies for an enhanced therapeutic index

Poster Monday, April 8
1:30 – 5:00pm PT

Presenter: Steve Wedge, Newcastle University, Newcastle upon Tyne, UK

3333
View Source!/20272/presentation/5680
ASTX295 is an oral, potent inhibitor of the p53-MDM2 protein-protein interaction that was discovered by Astex using its proprietary structure-based drug design approach. The compound was specifically designed to overcome the on-target toxicity seen in the first generation MDM2 antagonist compounds which have shown dose-limiting haematological toxicities in the clinic. In contrast, ASTX295 is a potent MDM2 antagonist with a clean CYP/hERG profile and a shorter human half-life allowing for pulsatile pathway modulation while avoiding myelosuppression. ASTX295 therefore has bone-marrow sparing characteristics which permit a differentiated safety profile to be presented at AACR (Free AACR Whitepaper). Astex is interested in discussing the further development of ASTX295 with potential partners.