• The preclinical data supports the clinical development of BBT-207 for EGFR mutant NSCLC patients harboring C797S double mutations, as well as for those who are treatment-naïve
• The company plans to submit an IND application to the US FDA in 2022 and looks forward to entering the Phase 1 study in 2023

SEONGNAM, South Korea, April 13, 2022 /PRNewswire/ -- Bridge Biotherapeutics (KQ288330), a South Korean clinical-stage biotechnology company focused on developing novel drugs for cancer, fibrosis and inflammation, announced that the preclinical data poster of BBT-207 was unveiled at the American Association for Cancer Research (AACR) 2022 being held from April 8-13.

BBT-207, a novel fourth-generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor (EGFR TKI) currently under IND-enabling preclinical development, is the company's first internally discovered drug candidate with potent activity and efficacy against a broad range of EGFR mutations in non-small cell lung cancer (NSCLC), including C797S double mutations which arise after third-generation EGFR TKI treatment.

During the poster presentation, the company highlighted the potent anti-tumor efficacy of BBT-207, observed through both in-vitro and in-vivo studies. Biochemical and cellular in-vitro efficacy data showed that BBT-207 is highly potent against EGFR C797S double mutations inclusive of Del19/C797S (DC) and L858R/C797S (LC) as well as driver mutations including Del19 and L858R. The results obtained from the in-vitro biochemical study demonstrated that the IC50 for EGFR tyrosine kinase inhibition activity was achieved at 0.8 nM against DC and LC double mutations, while Osimertinib showed 304.4 nM and 573.7 nM. Further, an in-vitro study utilizing Ba/F3 cell lines showed that BBT-207 is mutant selective and has minimal effect on wild-type EGFR.

The poster also highlighted the pharmacokinetics (PK) data of BBT-207 in animal models, which showed that the plasma concentrations of the drug candidate remained above the IC50 (0.7-11.8 ng/mL) and IC90 values (5.2-39.9 ng/mL, unpublished) for triple, double, and single mutations in Ba/F3 cell lines.

In addition, in-vivo efficacy studies have shown that BBT-207 boasts robust efficacy and induced tumor regressions over 14 days in both single (driver) mutations and C797S double mutations, when dosed at 40mg/kg QD. Further, BBT-207 demonstrated dose dependent tumor regression efficacy against T790M double mutations, which indicates the potential of BBT-207 as a broad-spectrum frontline treatment for NSCLC.

"We are highly encouraged that our data presented at the AACR annual meeting strongly supports that BBT-207 has the potential to be positioned as the best-in-class fourth-generation EGFR TKI targeting C797S double mutations as well as an advanced frontline treatment for EGFR-driven NSCLC," and "while third-generation EGFR TKIs are emerging as early-stage treatments, unmet medical needs relating to C797S mutations still exist. We look forward to entering the Phase 1 clinical study in metastatic NSCLC patients who harbor C797S mutations, in order to bring a novel therapy in the advanced cancer disease area," stated Jimmy Jin M.D., Ph.D., the Head of Discovery Biology of Bridge Biotherapeutics.

Bridge Biotherapeutics is also developing BBT-176, a fourth-generation EGFR TKI candidate that is designed to inhibit C797S triple mutations. As third-generation EGFR TKIs, such as Osimertinib, have emerged as first-line treatments for EGFR-mutant NSCLC, Bridge Biotherapeutics has reinforced its oncology pipelines by nominating BBT-207 in November 2021, as the first internally-discovered EGFR TKI inhibiting C797S double mutations. Armed with BBT-176 and BBT-207, the company aims to offer NSCLC patients comprehensive treatment solutions.

A copy of the poster presented at the AACR 2022 annual meeting is available at: https://bit.ly/3O4xOJp

The details of the presentation are as follows:

Presentation Title: BBT-207, a 4th Generation EGFR TKI With Broad-Spectrum Activity to Both Treatment-Emergent and Drug- naïve Mutants for the Treatment of NSCLC 

Session Category: Experimental and Molecular Therapeutics 

Session Title: Tyrosine Kinase and Phosphatase Inhibitors (PO.ET06.01) 

Session Date & Time: Tuesday, April 12, 2022, 1:30 pm -- 5:00 pm

Abstract Number: 3346 

About Bridge Biotherapeutics, Inc.

Bridge Biotherapeutics Inc. is a publicly traded clinical-stage biotech company based in the Republic of Korea with offices in the U.S. and China. Founded in 2015, Bridge Biotherapeutics is engaged in the discovery and development of novel therapeutics for disease indications with high unmet medical including cancer, ulcerative colitis, and fibrotic diseases. The company's pipeline includes BBT-401, a first-in-class Pellino-1 inhibitor for the treatment of ulcerative colitis; BBT-877, a novel autotaxin inhibitor for the treatment of fibrotic diseases including idiopathic pulmonary fibrosis (IPF); and BBT-176, a potent targeted cancer therapy for non-small cell lung cancer (NSCLC) with C797S triple EGFR mutations. For more information, visit https://www.bridgebiorx.com/en/.