Bright Future for Epigenetic Inhibitor Development from This Agreement


As a part of a broader agreement with Indian biotechnology firm Jubilant Biosys, TG Therapeutics (New York) entered into a sublicense agreement with Checkpoint Therapeutics for the development and commercialization of Jubilant’s novel BET inhibitor program for hematological malignancies.

jubilant biosys-TG-therapeutics-checkpoint inhibitor

As terms of the agreement following conditions were set:

  • Checkpoint Therapeutics will develop and commercialize these BET inhibitor molecules for solid tumors.
  • TG Therapeutics will pay an upfront licensing fee of $ 1 million plus additional contingency on achievement of certain milestones that accounts to a total payment of approximately $ 177 million,
  • TG Therapeutics will also fund various targeted research efforts at Jubilant Biosys.

Michael Weiss, Executive Chairman, interim CEO and president of TG Therapeutics stated “Epigenetic targeted agents, especially BET inhibitors, have been an area of great interest of ours for some time and are particularly attractive to us because of their effects on c-Myc driven tumors, like aggressive GCB-subtype DLBCL, an area we have seen early activity with TGR-1202 and our proprietary combination referred to as TG-1303. We want to thank our collaborators at Checkpoint for introducing us to this opportunity.

Weiss continued, “As we prepare to launch our registration directed studies in DLBCL and Follicular Lymphoma, we continue to look toward next steps in the evolution of patient care and believe the best outcome will be achieved only through the combination of multiple novel agents“.

BET inhibitors are a class of drugs that have shown certain anticancer and immunosuppressive effects in clinical trials.These are a widely researched class of drugs. They bind the bromodomain of Bromodomain and Extra Terminal (BET) motif proteins reversibly thus preventing protein protein interactions between BET proteins and acetylated histones. In mouse models of sepsis, these have prevented death. These drugs are also seen to attenuate autoimmunity and lessen damage from overactive inflammatory response in lungs.

brd4 mechanism

Figure 1. The mechanistic basis for transcriptional regulation by BRD4 (Photo credit: Adapted from Nat Rev Drug Discov 13(5): 337-356.)

Jubilant holds an exclusive, worldwide license for BET inhibitor program. Checkpoint “in-licenced” a group of patents that cover the compounds which inhibit BRD4, a member of the BET domain to be further developed for cancer treatment.

Regarding BET inhibitors, Weiss said “We are very excited to add this BET inhibitor program to our growing portfolio of agents targeting hematological malignancies. BET inhibitors have shown early promise in the treatment of relapsed and refractory Non-Hodgkin lymphomas, which remains a significant area of unmet medical need. There is emerging preclinical data showing BET inhibitors may enhance the activity of immuno-oncology agents, such as anti-PD-1/PD-L1 antibodies, providing multiple opportunities for us to combine this novel mechanism within our portfolio”.

Featured image credit: dna epigenetics and genetics mechanism symbol.  © Mikael Miro (Stock Photo ID: 117841184)

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