Preclinical data of Genhouse’s SHP2 inhibitor presented at AACR by HUYABIO

On April 11th 2022, Genhouse Bio, a biotech company focusing on development of next-generation small molecule therapeutics, announced today part of the preclinical data of its SHP2 inhibitor GH21 (HBI-2376) will be presented as a poster (Abstract # 5691) during the 2022 American Association for Cancer Research Annual Meeting (AACR 2022) by Genhouse’s strategic partner HUYABIO.

The published results show that GH21 displays greater potency as compared to TNO-155 and RMC-4550 in multiple CDX/PDX models with KRAS or EGFR mutations. In the MC38 syngeneic mouse model, GH21 demonstrates great synergy when combined with anti-PD1, which suggests its role in promoting anti-tumor immune response. GH21 can effectively inhibit the phosphorylation of  downstream ERK and the expression of DUSP6, making p-ERK and DUSP6 potential biomarkers of the target engagement and response to GH21.

At present, phase I clinical trials of GH21 (HBI-2376) have been initiated in both China and the U.S. The clinical development in the U.S is led by Genhouse’s strategic partner HUYABIO. In July 2020, HUYABIO and Genhouse entered into an exclusive license agreement, in which Genhouse licensed the ex-China development and commercialization right of GH21 to HUYABIO for $282M of upfront and milestone payments plus royalty.

Dr. Kuifeng Wang, the founder and CEO of Genhouse said, “GH21 is a SHP2 inhibitor independently developed by Genhouse. In preclinical studies, it has shown good efficacy in multiple solid tumor models with different mutations. At the same time, GH21 shows good safety profile and high oral bioavailability. It is expected to bring new treatment options for solid tumor patients with KRAS or EGFR mutations. We look forward to presenting the clinical data of GH21 from its phase I/II studies at international meetings in the near future.”

About SHP2

SHP2, also known as Tyrosine-protein phosphatase non-receptor type 11 (PTPN11), is the first oncogenic tyrosine-protein phosphatase discovered in history. Recently, SHP2 has drawn broad attention. On one hand, it is at the downstream of most RTK pathways, transducing cell proliferative and survival signals for RAS-MAPK/PI3K-mTOR pathway. On the other hand, SHP2 is also at the downstream of multiple immune checkpoints, such as PD-1 and BTLA, transducing immune escape signal in cancer cells, which gives SHP2 broad combo potential with immune checkpoint inhibitors. Therefore, SHP2 inhibitors are believed to have dual effects in both the RTK pathways and immune oncology.

About GH21

GH21 is a SHP2 allosteric inhibitor developed independently by Genhouse with global IP rights. GH21 has very high selectivity and is effective against multiple SHP2 point mutants. Both in vitro and in vivo studies have shown that GH21 does not affect any other tyrosine-protein phosphatases besides SHP2, thus has very low off-target risk. Moreover, GH21 has very good PK and safety profile, and a broad therapeutic window. Therefore, GH21 is a very promising small molecule drug candidate.

About Genhouse

Genhouse Bio is a clinical-stage biotech company focusing on the development of global next-generation anti-cancer therapeutics, headquartered in the Suzhou Industry Park . The senior management team of Genhouse has multiple years of experience in new drug development, clinical research and corporate management. Genhouse has a clear focus on original innovation and overcoming those “undruggable” targets.

Genhouse has established integrated in-house drug development platforms. With these platforms, Genhouse has started to build a highly innovative anti-cancer pipeline and out-licensed the ex-China rights of its SHP2 inhibitor GH21 to HUYABIO, an international biotech company. Genhouse will continue to advance more innovative pipeline programs into global development.

About HUYABIO International

HUYABIO is the leader in accelerating the global development of novel biopharmaceutical product opportunities originating in China enabling faster, more cost-effective and lower-risk drug development in the global markets. Through extensive collaboration with biopharmaceutical, academic and commercial organizations, it has built the largest China-sourced compound portfolio covering all therapeutic areas. With offices in the US, Japan, South Korea, Canada, Ireland and eight strategic locations across China, the Company has become a partner of choice to accelerate product development and maximize value globally. For more information, please visit www.huyabio.com.