[IL2102] SOS1 Inhibitor for RAS Driven Cancers 

• Potentially best-in-class, orally available, small molecule SOS1 inhibitor for any RAS driven cancers which has shown strong activity against various KRAS mutants and wild types including KRAS G12C, G12D, G12V and KRAS G13C. 

•  SOS1 is a pivotal switch that converts RAS from its inactive (off) state to its active (on) state, representing a novel therapeutic target in RAS-driven cancers Inhibition of the GTP exchange factor (GEF) SOS1-KRAS interaction impairs oncogenic signaling independently of the specific KRAS mutations; pan-KRAS inhibitor.

• IL2102 exhibited excellent PK profiles both in rodents and non-rodents and low plasma protein binding, offering high unbound drug concentration.

• IL2102 has demonstrated significant in vivo activity as a single agent in a lung tumor xenograft model (G12C sensitive). Additionally, combination of IL2102 with a KRAS G12C inhibitor led to a significant synergistic anti-tumor activity, resulting in complete tumor regression in all animals of the combination groups (24 out of 30 animals) with favorable safety profile (no deaths observed in all 30 animals), in a dose dependent manner.

• IL2102 can be developed as a combination agent with any type of KRAS inhibitors (specific mutation or pan-type) due to its broad activity profile in most type of KRAS mutants and wild types.

• This candidate is ready for IND-enabling GLP toxicity studies.