A Novel HDAC6 Inhibitor, MPT0G211, for Cancer Treatment
MPT0G211 is a highly selective small molecular against HDAC6 with the best pharmacological profile.
Targeted indication
• Multiple Myeloma (MM)
• Glioblastoma
Status
In pre-clinical studies ; Expect to file FDA IND in Q4 2023
Key features
- MPT0G211 is a highly selective small molecular against HDAC6 with the best pharmacological profile.
- MPT0G211 strongly inhibits tumor growth in multiple cancer types, especially in multiple myeloma and glioblastoma.
- MPT0G211 shows promising safety profile in rat and dog.
Market
Multiple myeloma remains an incurable disease even though it is becoming more manageable. The treatment of MM has changed dramatically in recent years, with the introduction of new drugs into therapeutic strategies, both in the front line setting and in relapsed refractory disease. However, most patients eventually relapse and often demonstrate multiple drug resistance. Although MM only account for less than 2% of cancer, the therapeutic market is among the highest due to aging population, prolong survival and treatment duration.
MODE OF ACTION
• MPT0G211 selectively inhibits class II HDAC6 with IC50 values of 0.291 nM, when compared to other class HDACs more than 1000 - 42000 folds.
• When combined with Bortezomib, MPT0G211 significantly inhibited cell proliferation in multiple myeloma cell lines without effect on normal bone marrow cells.
EXPERIMENTAL RESULTS
MPT0G211 only induced a-tubulin acetylation without affecting nuclear proteins histone 3 and histone 4 even at high dose level.
• MPT0G211 dose-dependently inhibited tumor growth
• When combined with current drugs, MPT0G211 synergistically inhibited tumor growth in animal studies.
• Already completed CMC for drug substance
• Already completed CMC for drug product
• Already completed ADME studies
• No MPT0G211-related changes were detected in rats with MTD > 1000 mg
• No apparent MPT0G211-related changes in dogs.
• Did not induced significant effects on CV, respiratory or CNS system.
INTELLECTUAL PROPERTY
SELECTED PUBLICATIONS
• J Med Chem. 2018 Feb 8;61(3):905-917.
• BBA Mol Cell Res. 2019 Jun;1866(6):992.
• Clin Epigenetics. 2018 Dec 29;10(1):162.
• Cell Death Dis. 2018 May 29;9(6):655
BUSINESS OPPORTUNITY
License or co-development after IND or phase 1 study
CONTACT
service@biip-dcc.org