BTX-1188 / BioTheryX - LARVOL DELTA

A Study of BTX-1188 in Subjects With Advanced Malignancies (clinicaltrials.gov) - P1 | N=8 | Terminated | Sponsor: BioTheryX, Inc. | N=168 ➔ 8 | Trial completion date: May 2026 ➔ Sep 2023 | Recruiting ➔ Terminated | Trial primary completion date: Apr 2025 ➔ Sep 2023; Business decision

Enrollment change • Metastases • Trial completion date • Trial primary completion date • Trial termination • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Solid Tumor

Biotheryx to Present Preclinical Findings on Protein Degrader Programs at 5th Annual Targeted Protein Degradation Summit (PRNewswire) - "Biotheryx, Inc...announced that it will present preclinical data from its targeted protein degrader programs at the 5th Annual Targeted Protein Degradation Summit, being held October 25-28, 2022, in Boston, Massachusetts....Leah Fung, Ph.D., Chief Scientific Officer of Biotheryx, will present as a Keynote Plenary Speaker in a session...to highlight novel small molecule bifunctional degraders of son of sevenless homolog 1 (SOS1), potent inhibitors of Kirsten rat sarcoma (KRAS) mutant cancers. Aparajita Chourasia, Ph.D., Vice President of Biology of Biotheryx will also present the latest preclinical data in support of the Company's BTX-1188 molecular glue program targeting GSPT1 and IKZF1/3."

Preclinical • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Oncology • Sarcoma • Solid Tumor

A Study of BTX-1188 in Subjects With Advanced Malignancies (clinicaltrials.gov) - P1; N=168; Recruiting; Sponsor: BioTheryX, Inc.; Not yet recruiting ➔ Recruiting

Enrollment open • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Solid Tumor • MRI

Targeting cereblon in hematologic malignancies. (PubMed, Blood Rev) - "This review describes novel thalidomide analogs, immunomodulatory drugs, also known as CRBN E3 ubiquitin ligase modulators or molecular glues (avadomide, iberdomide, CC-885, CC-90009, BTX-1188, CC-92480, CC-99282, CFT7455, and CC-91633), and CRBN-based proteolysis targeting chimeras (PROTACs) with increased efficacy and potent activity for application in hematologic malignancies...Proteins that are traditionally difficult to target (transcription factors and oncoproteins) can be polyubiquitinated and degraded in this way. The competition of CRBN neosubstrates with endogenous CRBN-interacting proteins and the pharmacology and rational combination therapies of and mechanisms of resistance to CRL4 modulators or CRBN-based PROTACs are described."

Journal • Review • Hematological Disorders • Hematological Malignancies • Immune Modulation • Inflammation • Oncology • Targeted Protein Degradation • CRBN • IL17RB

BTX-1188, a first-in-class dual degrader of GSPT1 and IKZF1/3, for treatment of acute myeloid leukemia (AML) and solid tumors. (ASCO 2022) - "This approach is expected to improve clinical outcomes and reduce toxicities associated with pure GSPT1 degradation (CC-90009), thus expanding the therapeutic window of BTX-1188. Functionally, BTX-1188 is cytotoxic in various cancer cell lines such as Myc-driven lines (IC50 range: 0.5-10 nM) and primary human AML patient samples (IC50 range: 0.4-1.5 nM), including relapsed/refractory-, cytarabine- and venetoclax-resistant samples... These preclinical data show that BTX-1188 is a promising drug candidate for AML and other tumor types. Its immunomodulatory properties owing to IKZF1/3 degradation may prevent systemic inflammatory dose-limiting toxicities associated with pure GSPT1 degradation (Uy 2019). BTX-1188 has entered phase 1 clinical studies for advanced solid tumors and AML."

Acute Myelogenous Leukemia • Diffuse Large B Cell Lymphoma • Hematological Disorders • Hematological Malignancies • Immune Modulation • Inflammation • Leukemia • Lung Cancer • Lymphoma • Non Small Cell Lung Cancer • Non-Hodgkin’s Lymphoma • Oncology • Solid Tumor • Targeted Protein Degradation • CRBN • GSPT1 • IKZF1 • IL1B • IL2 • IL6 • TNFA

A Study of BTX-1188 in Subjects With Advanced Malignancies (clinicaltrials.gov) - P1; N=168; Not yet recruiting; Sponsor: BioTheryX, Inc.

Clinical • New P1 trial • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Solid Tumor • MRI

BioTheryX Doses First Patient in Phase 1 Study Investigating Lead Protein Degrader Candidate BTX-1188 (PRNewswire) - "BioTheryX...announced dosing of the first patient in a new, first-in human Phase 1 study investigating its lead candidate BTX-1188, an oral, dual target protein degrader specifically engineered to degrade GSPT1 and IKZF1/3, in patients with advanced hematologic and solid tumor malignancies....The Phase 1 clinical trial is a multicenter, open label, non-randomized, sequential dose escalation study to assess the safety, pharmacokinetics and preliminary efficacy of BTX-1188 in patients with acute myeloid leukemia, advanced lymphoid and solid tumors who have failed standard therapy."

Trial status • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Oncology • Solid Tumor

BioTheryX Receives IND Clearance from FDA to Proceed with Phase 1 Study of BTX-1188, a Molecular Glue, for the Treatment of Hematologic and Solid Malignancies (PRNewswire) - "BioTheryX, Inc...announced that the U.S. Food and Drug Administration (FDA) cleared the company to proceed with a Phase 1 clinical trial of BTX-1188 in hematologic and solid malignancies...'We plan to study BTX-1188 in patients with hematological and solid malignancies who have limited treatment options and for whom new therapies are desperately needed. We expect to initiate patient enrollment in the Phase I study by year end.'"

Enrollment status • IND • Hematological Malignancies • Oncology • Solid Tumor

BioTheryX Announces $92M Series E Financing to Accelerate Development of Targeted Protein Degradation Pipeline and Technology Platform in Oncology (PRNewswire) - "BioTheryX, Inc...announced a $92 million Series E financing led by Farallon Capital Management...The proceeds from the financing will be used to advance...BTX-1188, toward clinical development. BioTheryX also plans to advance the clinical development of its lead multi-kinase inhibitor, BTX-A51, for the treatment of acute myeloid leukemia, myelodysplastic syndromes and solid tumors....'With this financing, we are well positioned to execute our plans to bring our first molecular glue program BTX-1188 into the clinic by the end of 2021, expand our platform of molecular glues, PROTACs and monovalent degraders and progress our lead program BTX-A51 through Phase 1.'"

Clinical • Financing • Acute Myelogenous Leukemia • Hematological Malignancies • Myelodysplastic Syndrome • Oncology • Solid Tumor