Apabetalone

(RVX-208)

Resverlogix

Oral

Phase III

Coronary artery disease

BETonMACE is a global Phase III study in patients with type 2 diabetes and coronary artery disease, investigating the ability of Apabetalone to reduce the risk of major adverse cardiovascular events. Top-line results can be expected in H219. We note that Apabetalone binds preferentially (c 20-fold) to the second binding domain (BD2), as opposed to NUE20798, which binds preferentially to BD1 (>100-fold selective).

BMS-986158

Bristol-Myers Squibb

Oral

Phase I/II

Cancer

Currently in a Phase I/II development investigating it as both a monotherapy and in combination with BMS’s PD-1 inhibitor Opdivo (nivolumab) for the treatment of cancer. Interim data was presented at ESMO2018 that showed it was generally well tolerated as a monotherapy with thrombocytopenia being the only dose-limiting toxicity.

INCB057643

Incyte

Oral

Phase I/II

Cancer

Completed Phase I/II study (December 2018) in patients with a range of advanced solid tumours and hematologic malignancies. Preliminary results from the trial were presented at ASH2017 and showed the maximum tolerated dose was established in the Phase I study at 12mg qd. Expanded Phase II cohorts are investigating treatment as a monotherapy and in combination with standard of care treatments; complete data are yet to be published.

GSK525762

GlaxoSmithKline

Oral

Phase II

Cancer

Under investigation in multiple Phase II studies for various indications.

RG6146

(TEN-010)

Roche/Tensha

Oral

Phase Ib

Cancer

Currently in two Phase Ib clinical trials in patients with various hematologic malignancies, investigating its use as a monotherapy and in combination with other standard of care treatments.