Daiichi Sankyo Company, Limited

National Cancer Center

Saito Higuchi

Jun Watanabe

Hiroyuki Naito

Kentaro Ito

Masao Itoh

Hiroaki Inagaki

Yoshiko Kagoshima

Yuichi Tominaga

Biswajit Das

Katsuhiro Kobayashi

Tetsunori Fujisawa

Aki Yokomizo

Toshifumi Tsuda

Rita Katoch

Ryutaro Kanada

Takashi Kohno

Dilip J Upadhyay

Makoto Haruta

Akifumi Nakamura

Takashi Suzuki

Hideaki Funami

Masayoshi Asano

Akiko Egami

Hideaki Ogiwara

The present invention provides a compound having excellent histone acetyl transferase inhibitory activity against EP300 and/or CREBBP, or a pharmacologically acceptable salt thereof. The compound is represented by the following formula (1) or a pharmacologically acceptable salt thereof: 

EP300/CREBBP inhibitor

It has been found that CBP and p300 are in the relationship of synthetic lethality, and treatment inhibiting p300 is a promising approach for the treatment of CBP-mutated cancer. It has also been revealed that this therapeutic strategy achieves efficient treatment based on companion diagnostics because a p300 inhibitor can be administered to a cancer patient selected with functional suppression of CBP as an index.

Method for predicting responsiveness to cancer treatment using p300-inhibiting compound

A compound represented by the following formula (I) or a salt thereof:   

Amino group-containing pyrrolidinone derivative

Growing community of inventors

Koto-ku, Japan

Saito Higuchi