Won Sik Lee

Abstract Bosmolisib is a novel triple inhibitor of PI3K-δ/γ and DNA-PK for malignancy treatment. This was a first-in-human, phase 1, open-label, dose-escalation, and dose-expansion trial with relapsed/refractory (R/R) non-Hodgkin lymphoma (NHL). Patients received bosmolisib orally once daily in 28-day cycles across four dose levels (50–325 mg) until disease progression or unacceptable toxicity.

1 Introduction The poly (ADP-ribose) polymerase (PARP) is a ubiquitous nuclear enzyme involved in DNA repair. It catalyzes the transfer of ADP-ribose to target proteins (PARylation) by utilizing nicotinamide adenine dinucleotide (NAD+) [1]. Among the 17 PARP family members, PARP-1 and PARP-2 are involved in DNA damage repair and are essential for cell survival [2]. Many proteins are involved in the DNA damage response (DDR), which can be affected by alterations in those proteins.