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Catalyst Info & Data Links
TITLE: Umbralisib Monotherapy in Relapsed/Refractory Marginal Zone Lymphoma (MZL) and Follicular Lymphoma (FL)
WHAT IS THE CATALYST EVENT?
Year-end-2020: Full Data Presentation
WHEN WILL THE EVENT (OR DID THE EVENT) OCCUR?
2016: Differential regulation of human T-cells by TGR-1202, a novel PI3Kδ inhibitor. Cancer Res, 76 (14 Supplement), 545.
2017: Umbralisib/TGR-1202 As a Novel Dual PI3K/CK1 Inhibitor Has a Unique Therapeutic Role in Silencing Oncogenes in Aggressive Lymphomas. Blood, 130(Supplement 1), 2809-2809.
2019: Umbralisib monotherapy demonstrates efficacy and safety in patients with relapsed/refractory marginal zone lymphoma: a multicenter, open-label, registration directed phase 2 study. Hematol Oncol, 37(S2), 182-183.
2019: Umbralisib Monotherapy Demonstrates Efficacy and Safety in Patients with Relapsed/Refractory Marginal Zone Lymphoma: A Multicenter, Open-Label, Registration Directed Phase 2 Study (International Congress on Malignant Lymphoma)
2019: Umbralisib monotherapy demonstrates efficacy and safety in patients with relapsed/ refractory marginal zone lymphoma: a multicenter, open-label, registration directed phase 2 study (American Society of Clinical Oncology Annual Meeting)
2020: J.P. Morgan Healthcare Conference (slides 5-11)
REVLIMID® (lenalidomide) - Celgene Corp
~22,500 new cases per year in MZL and FL
~6,000-10,0002 relapsed indolent patients needing treatment each year
source - 2020 J.P. Morgan Healthcare Conference (slide 10)
MECHANISM OF ACTION / RATIONALE
Umbralisib (TGR-1202) is an oral, once daily, dual inhibitor of PI3K delta and CK1 epsilon. The phosphoinositide-3-kinases (“PI3Ks”) are a family of enzymes involved in various cellular functions, including cell proliferation and survival, cell differentiation, intracellular trafficking, and immunity. There are four isoforms of PI3K (alpha, beta, delta, and gamma), of which the delta isoform is strongly expressed in cells of hematopoietic origin, and often implicated in B-cell related lymphomas.
Umbralisib has nanomolar potency to the delta isoform of PI3K and high selectivity over the alpha, beta, and gamma PI3K isoforms. Umbralisib also uniquely inhibits casein kinase 1 epsilon (CK1 epsilon), which may have both direct anti-cancer effects and may also modulate T-cell activity associated with immune-mediated adverse events seen with previous PI3K inhibitors. Currently approved PI3K delta inhibitors have been associated with autoimmune mediated toxicities such as liver toxicity, lung toxicity and colitis. We believe the specificity differences of umbralisib, as compared to the approved PI3K inhibitors, its unique inhibition of CK1 epsilon, as well as its distinct and patented chemical structure may differentiate umbralisib within the PI3K inhibitor class.
Updated by HC
TGTX, UNITY-NHL, Umbralisib Monotherapy, Marginal Zone Lymphoma (MZL), Follicular Lymphoma (FL)
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