Next-generation RAF inhibitor to file for IND and Fast Track designation in the U.S.

On February 14, Xynom announced that it has successfully completed the pre-IND meeting with the US FDA and will submit a global multi-center clinical trial of its drug candidate, XP-102, a broad-spectrum RAF inhibitor, to the FDA in the first quarter of 2022.

According to public information, XP-102 is a potent, highly selective, inactive conformation (DFG-out) RAF inhibitor, which was acquired by Xynom Pharma from Boehringer Ingelheim with a total value of about US$500 million.

According to the press release, XP-102 has comparable inhibitory activity and binding potency to B-RAF (V600E), B-RAF wild-type and C-RAF, and has certain differentiated advantages, such as a unique DFG-out conformation, a wider Therapeutic window, more pronounced and longer-lasting inhibition of RAF signaling pathway, and stronger tumor-suppressive effect in comparative experiments

In multiple mouse pharmacodynamic experiments, XP-102 has shown good development potential, including: 1) Combination with cetuximab can shrink tumors in HT-29-resistant colorectal cancer models; 2) Combined with Xynom's third-generation mTORC1/2 inhibitor XP-105 in the treatment of colorectal cancer, showing a good tumor inhibition effect in mice; 3) With Shanghai Kezhou Pharmaceutical's MEK inhibitor HL The combination of -085, in the treatment of drug-resistant colorectal cancer and melanoma, achieved tumor growth inhibition rates of 98.

According to the press release, the applied global multi-center clinical Phase 1/2a clinical trial will be mainly conducted in the United States and China

references:

[1] Xynow Pharmaceuticals will apply for 2 new FDA Fast Track designations! A new generation of RAF inhibitors will initiate a phase 12a global multicenter trial.

[2] Xynomic Pharma acquired Boehringer Ingelheim’s innovative and potent PAN-RAF inhibitor BI 882370 for a total value of US$502 million.