JBI-802 / Jubilant Pharmova - LARVOL DELTA

Anti-tumor activity of CoREST inhibitor, JBI-802 (dual epigenetic modifier of LSD1/HDAC6): An opportunity to treat essential thrombocythemia and MPN/MDS patients with thrombocytosis in ongoing phase 1/2 clinical trial. (ASCO 2025) - P1/2 | "Clinical Trial Registration Number: ACTRN12624000478516 The abstract will be released to the public on May 22, 2025 at 4:00 PM"

Clinical • P1/2 data • Essential Thrombocythemia • Hematological Disorders • Myelodysplastic Syndrome • Myeloproliferative Neoplasm • Oncology • Thrombocytosis

Phase 1/ Phase 2 Study to Assess Safety and Efficacy of Orally Administered JBI-802 in Subjects with Myeloproliferative Neoplasms (MPN) and Myelodysplastic/Myeloproliferative Neoplasms (MDS/MPN) with Thrombocytosis. (ANZCTR) - P1/2 | N=30 | Recruiting | Sponsor: Jubilant Therapeutics, Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • Essential Thrombocythemia • Hematological Disorders • Hematological Malignancies • Myelodysplastic Syndrome • Myeloproliferative Neoplasm • Oncology • Thrombocytosis

Genetic differences between primary and metastatic Ewing Sarcoma: implications for targeted therapeutics (PAS 2025) - "Upstream regulators include beta-estradiol, TGFB1, dexamethasone, TBX3, and ERBB2. Top upregulated genes in metastatic ES compared to primary ES tumors include ZNGE1, SFTA3, and SFTPC. Down regulated genes include OGN, CXCL14, and COMP which are genes that contribute to osteoblast differentiation, maintenance of macrophages, and proteins in the extracellular matrix. Extracellular matrix formation (z-score -3.000), assembly of collagen fibrils (-3.207), and integrin cell surface interactions (-2.324) are top canonical pathways with predicted inhibition."

Metastases • Ewing Sarcoma • Lung Cancer • Oncology • Osteosarcoma • Sarcoma • Solid Tumor • CXCL14 • HER-2 • SFTA3 • TBX3 • TGFB1

JBI-802: the first orally available LSD1/HDAC6 dual inhibitor to enter clinical trials. (PubMed, Expert Opin Ther Pat) - "JBI-802 is currently undergoing phase I/II clinical trials in patients with advanced solid tumors, myeloproliferative neoplasms (MPN), and myelodysplastic/myeloproliferative neoplasms (MDS/MPN) with thrombocytosis. However, the potential on-target toxicity, off-target interactions and selectivity concerns are deserved more attention."

Journal • Review • Hematological Disorders • Hematological Malignancies • Myelodysplastic Syndrome • Myeloproliferative Neoplasm • Oncology • Solid Tumor • Thrombocytosis

JBI802 a Highly Potent Corest Inhibitor Demonstrated Anti-Tumor Activity at Low Dose, Thrombocytopenia at Higher Dose NOW Leading to an Opportunity to Treat ET Myeloproliferative Neoplasms (MPN) /Essential Thrombocythemia [ET]) and Myelodysplastic/Myeloproliferative Neoplasms (MDS/MPN) with Thrombocytosis (ASH 2024) - P1/2 | "Based on these data, there is a strong scientific rationale to test the activity of JBI-802 in diseases such MPN and MDS/MPN with thrombocytosis representing an advantage over currently available therapies. As the study progress, interim data from the phase 1/2 clinical trial of ET and MPN patients will be presented."

Anemia • Essential Thrombocythemia • Hematological Disorders • Hematological Malignancies • Lung Cancer • Myelodysplastic Syndrome • Myeloproliferative Neoplasm • Oncology • Pain • Solid Tumor • Thrombocytopenia • Thrombocytosis

Jubilant Therapeutics Inc. announces First Patient Dosing in Global Clinical Trials for JBI-802, a CoREST Inhibitor and JBI-778, a PRMT5 Inhibitor (PRNewswire) - "Jubilant Therapeutics Inc...announced the dosing of first patients in global clinical trials involving two pipeline programs: Phase I/II clinical trial of JBI-802 in heme-oncology and Phase I clinical trial for JBI-778 in solid tumors....The second clinical trial is to assess both safety and the recommended Phase II dose for JBI-778, an oral brain-penetrant inhibitor of PRMT5 (Protein arginine N-methyltransferase 5) in mEGFR Tyrosine Kinase Inhibitor (TKI) resistant NSCLC, IDH+ high-grade glioma (HGG) and Adenoid Cystic Carcinoma (ACC)."

Trial status • Adenoid Cystic Carcinoma • Essential Thrombocythemia • Glioma • Myelodysplastic Syndrome • Myeloproliferative Neoplasm • Non Small Cell Lung Cancer

Phase 1/ Phase 2 Study to Assess Safety and Efficacy of Orally Administered JBI-802 in Subjects with Myeloproliferative Neoplasms (MPN) and Myelodysplastic/Myeloproliferative Neoplasms (MDS/MPN) with Thrombocytosis. (ANZCTR) - P1/2 | N=30 | Not yet recruiting | Sponsor: Jubilant Therapeutics, Inc.

New P1/2 trial • Essential Thrombocythemia • Hematological Disorders • Hematological Malignancies • Myelodysplastic Syndrome • Myeloproliferative Neoplasm • Oncology • Thrombocytosis

Combination Therapy and Dual-Target Inhibitors Based on LSD1: New Emerging Tools in Cancer Therapy. (PubMed, J Med Chem) - "Over two decades, numerous LSD1 inhibitors have been reported, especially some of which have entered clinical trials, including eight irreversible inhibitors (TCP, ORY-1001, GSK-2879552, INCB059872, IMG-7289, ORY-2001, TAK-418, and LH-1802) and two reversible inhibitors (CC-90011 and SP-2577)...LSD1 multitarget inhibitors have also been reported, exampled by clinical dual LSD1/histone deacetylases (HDACs) inhibitors 4SC-202 and JBI-802. Herein, we present a comprehensive overview of the combination of LSD1 inhibitors with various antitumor agents, as well as LSD1 multitarget inhibitors. Additionally, the challenges and future research directionsare also discussed, and we hope this review will provide new insight into the development of LSD1-targeted anticancer agents."

Combination therapy • Journal • Review • Oncology

JBI-802 initial Phase I data suggests therapeutic potential in sensitizing immunotherapy resistant tumors and in Myeloproliferative Neoplasms with thrombocytosis (PRNewswire) - P1 | N=126 | NCT05268666 | Sponsor: Jubilant Therapeutics Inc. | "Jubilant Therapeutics Inc...inhibitor JBI-802 with the dual activity on LSD1 and HDAC6, today announced preliminary safety, pharmacokinetic and initial efficacy results of the Phase I trial in advanced cancer patients...The data from first 11 patients with advanced cancer revealed a dose-proportional increase in exposure across cohorts and a strong correlation between the exposure and the on-target effects of platelet decrease, indicating that pharmacological relevant level of LSD1 inhibition have been achieved...JBI-802 from LSD1-only inhibitors. Specifically, no AEs (Adverse Events) of anemia has been observed, which is potentially due to the positive benefit of inhibition of HDAC6 in erythrocytes....JBI-802 showed a confirmed partial response in this IO-refractory NSCLC patient with a 39% decrease in the target lung tumor mass."

P1 data • Hematological Malignancies • Lung Cancer • Myeloproliferative Neoplasm • Non Small Cell Lung Cancer • Oncology • Solid Tumor

LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials. (PubMed, Front Pharmacol) - "Seven of them (tranylcypromine, iadademstat (ORY-1001), bomedemstat (IMG-7289), GSK-2879552, INCB059872, JBI-802, and Phenelzine) covalently bind the FAD cofactor, and two are non-covalent LSD1 inhibitors [pulrodemstat (CC-90011) and seclidemstat (SP-2577)]. Another TCP-based LSD1/MAO-B dual inhibitor, vafidemstat (ORY-2001), is in clinical trial for Alzheimer's diseases and personality disorders. The present review summarizes the structure and functions of LSD1, its pathological implications in cancer and non-cancer diseases, and the identification of LSD1 covalent and non-covalent inhibitors with different chemical scaffolds, including those involved in clinical trials, highlighting their potential as potent and selective anticancer agents."

Journal • Review • Acute Myelogenous Leukemia • Alzheimer's Disease • CNS Disorders • Esophageal Cancer • Gastrointestinal Cancer • Hematological Disorders • Hematological Malignancies • Leukemia • Mood Disorders • Oncology • Personality Disorder • Solid Tumor

"#JubilantTherapeutics Inc. receives #OrphanDrugDesignation for #JBI802 for #AcuteMyeloidLeukemia (#AML) and #SmallCellLungCancer (#SCLC) https://t.co/XaPYUxudFf" (@1stOncology)

Orphan drug • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Lung Cancer • Neuroendocrine Tumor • Oncology • Small Cell Lung Cancer • Solid Tumor

Jubilant Therapeutics Inc. receives Orphan Drug Designation for JBI-802 for Acute Myeloid Leukemia (AML) and Small Cell Lung Cancer (SCLC) (PRNewswire) - "Jubilant Therapeutics...announced that the United States Food and Drug Administration (US FDA) has granted Orphan Drug Designation for JBI-802 for the treatment of small cell lung cancer (SCLC) and acute myeloid leukemia (AML). JBI-802 is a dual epigenetic modulator engineered in a single pharmacophore to achieve optimal inhibition of the transcriptional regulator CoREST, which regulates the development of cellular lineages responsible for neuroendocrine tumors like SCLC and hematopoietic tumors like AML."

Orphan drug • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Lung Cancer • Oncology • Small Cell Lung Cancer • Solid Tumor • Thoracic Cancer

Jubilant Therapeutics Inc. Doses First Patient in Phase I/II Trial Evaluating JBI-802, dual inhibitor of LSD1 and HDAC6, in patients with advanced solid tumors (PRNewswire) - "Jubilant Therapeutics Inc...announced the dosing of the first patient in a Phase I/II clinical trial of JBI-802 in patients with advanced solid tumors....The Phase I/II trial is an open label, two-part dose escalation and expansion study designed to define the safety and tolerability, explore predictive biomarkers and assess preliminary activity of JBI-802 in more than 100 study participants with advanced solid tumors."

Trial status • Oncology • Solid Tumor

A Study of Orally Administered JBI-802, an LSD1/HDAC6 Inhibitor, in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1/2 | N=126 | Recruiting | Sponsor: Jubilant Therapeutics Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • Colorectal Cancer • Gastrointestinal Cancer • Hepatocellular Cancer • Lung Cancer • Oncology • Solid Tumor

A Study of Orally Administered JBI-802, an LSD1/HDAC6 Inhibitor, in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1/2 | N=126 | Not yet recruiting | Sponsor: Jubilant Therapeutics Inc.

New P1/2 trial • Colorectal Cancer • Gastrointestinal Cancer • Hepatocellular Cancer • Lung Cancer • Oncology • Solid Tumor

Jubilant Therapeutics Announces FDA Clearance of IND for JBI-802, a Novel Dual LSD1 and HDAC6 Inhibitor, for treatment of Solid Tumors (PRNewswire) - "Jubilant Therapeutics...today announced U.S. Food and Drug Administration (FDA) clearance of the investigational new drug application (IND) for JBI-802, a novel, oral, potent and selective dual inhibitor of LSD1 and HDAC6, for the treatment of small cell lung cancer (SCLC), treatment-induced neuro-endocrine prostate cancer (NEPC) and other mutation-defined neuroendocrine tumors."

IND • Genito-urinary Cancer • Lung Cancer • Neuroendocrine Tumor • Oncology • Prostate Cancer • Small Cell Lung Cancer • Solid Tumor

Jubilant Therapeutics Announces Successful Completion of Pre-IND Meeting with FDA for its Novel Dual LSD1 and HDAC6 Inhibitor JB1-802 (PRNewswire) - "Jubilant Therapeutics Inc...today announced the successful completion of a pre-IND (Investigational New Drug) meeting with the U.S. Food and Drug Administration (FDA) regarding the development plan, clinical study design and dosing strategy for the Phase I/II trial of JB1-802...for the treatment of small cell lung cancer, treatment-induced neuro-endocrine prostate cancer and other mutation-defined neuroendocrine tumors...'We are pleased with the outcome of the pre-IND meeting with the FDA and plan to submit the IND application by the end of 2021.'"

FDA event • IND • Oncology

Jubilant Therapeutics announces Efficacy and Biomarker Data at 62nd ASH Annual Meeting for its Novel Dual LSD1-HDAC6 Inhibitor for the Treatment of Hematological Cancers (PRNewswire) - "Both LSD1 and HDAC6 mechanisms are operational with JBI-802 resulting in stronger anti-proliferation and efficacy in a subset of cell lines; Selective biomarkers are modulated with the dual inhibition of JBI-802 not seen by the single agent inhibitors, leading to the potential for patient stratification and the evaluation of treatment response; and JBI-802 has a superior efficacy, safety and tolerability profile."

Preclinical • Acute Myelogenous Leukemia • Hematological Malignancies • Oncology

Jubilant Therapeutics Announces Upcoming Presentation at 2020 ASH Virtual Annual Meeting (PRNewswire) - “Jubilant Therapeutics Inc…announced that an abstract related to its dual LSD1 and HDAC6 inhibitor, JBI-802, has been accepted for presentation at the 62nd American Society of Hematology (ASH) Virtual Annual Meeting taking place Dec. 5-8, 2020….‘Our work to progress JBI-802 into the clinic as a potential, differentiated therapeutic for the treatment of select hematological and solid tumors with specific gene signatures is on track and we expect to initiate first-in-human studies in the second half of next year.’”

Clinical data • New trial • Hematological Malignancies • Oncology • Solid Tumor

[VIRTUAL] Novel Dual Inhibitor of LSD1-HDAC6/8 for Treatment of Cancer (ASH 2020) - "JBI-802 is currently being evaluated in IND-enabling studies to be progressed into clinical trials and such inhibitors could serve as powerful therapeutic agents for the treatment of specific cancers."

Hematological Malignancies • Oncology • HDAC1

Jubilant Therapeutics and OneThree Biotech Collaborate to Advance Precision Oncology (PRNewswire) - "Jubilant...today announced their collaboration and the successful completion of a study focused on the identification of specific biomarkers for new indications in targeted oncology patient populations...JBI-802 is currently being evaluated in IND-enabling studies for the treatment of hematological and select solid tumors with specific gene signatures and first-in-human clinical studies are expected in 2021."

Licensing / partnership • New trial