Rain Therapeutics Presents Preclinical Activity of Tarloxotinib in NRG1 Fusion Cancers at the Annual American Association for Cancer Research (AACR) Meeting

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Data support expanding clinical development of tarloxotinib to patients with NRG1 fusion and rearranged cancers with a tumor agnostic, basket strategy

NEWARK, Calif., April 2, 2019 — Rain Therapeutics Inc., a privately-held, clinical stage biotechnology company focused on biomarker-driven, small molecule therapeutics for patients with cancer, today announced that it presented new preclinical data on tarloxotinib (Tarlox), a hypoxia-activated pan-HER inhibitor, in NRG1 fusion positive cancers at the American Association for Cancer Research (AACR) Annual Meeting 2019, held in Atlanta, Georgia from March 29-April 3, 2019. These data support a potential addititional indication for Rain. Rain is currently conducting a Phase 2 clinical trial of Tarlox in EGFR Exon 20 and HER2 mutation positive non-small cell lung cancer.

“The activity observed by Tarlox in NRG1 fusion models is very exciting,” said Avanish Vellanki, chief executive officer of Rain Therapeutics. “The potency of tarlox observed across various in vitro and patient-derived animal studies was intuitive as NRG1 tumors rely on HER-signaling.”

Robert Doebele, MD, PhD, acting chief science officer of Rain Therapeutics continued, “NRG1 fusion positive cancers resemble NTRK fusion tumors in their addiction to a single oncogenic driver and their presence across multiple tumor types. Like EGFR and HER2 exon 20 insertion mutations, NRG1 fusions represent cancers that are difficult to drug without significant toxicity, hence providing another opportunity for the hypoxia-activated strategy of tarloxotinib.”  

NRG1 encodes the HER3 ligand neuregulin 1. NRG1 gene fusions are oncogenic drivers that overexpress the HER3 ligand, leading to heterodimerization of HER2/HER3 and activation of downstream ERK, PI3K–AKT and NF-kB pathways. NRG1 fusions are particularly enriched in invasive mucinous adenocarcinoma of the lung where they are found in 27-31% of cases and have also been reported in other cancer types with an overall incidence of 0.2% across all solid tumors. The preclinical studies presented at AACR demonstrate, among other significant findings, that Tarlox significantly inhibited tumor growth and regressed tumors in an NRG1 ovarian cancer patient-derived xenograft model. There was a 100% reduction in tumor size in the group dosed with 48 mg/kg of Tarlox as compared to a 150% increase in tumor size in the control group.

Data from the preclinical study were presented in a poster entitled “Tarloxotinib Exhibits Potent Activity in NRG1 Gene Fusion Positive Cancers.” A copy of the presentation materials can be accessed by visiting the Publications section of the Rain website.

About Rain Therapeutics Inc.

Rain Therapeutics Inc. is a privately-held biotechnology company developing biomarker-driven small molecule therapeutics for patients with cancer. Rain’s lead program, Tarloxotinib, is a hypoxia-activated prodrug of a potent pan-ErbB inhibitor in development as a treatment for non-small cell lung cancer patients with EGFR / ErbB Exon 20 insertion mutations. Rain Therapeutics Inc. has worldwide development and commercialization rights for Tarloxotinib. For more information, visit www.rainthera.com

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