Science at Aurigene

Protein degraders are powerful tools to chemically silence targets of interest including those that are previously considered undruggable. Being an early adopter, our unique platform accelerates the identification of these degraders with zero or minimal linker between ligands of E3 ligase and target proteins.

One of the examples, AU-15330 is a SMARCA2/4 selective tool degrader created using the platform. With one of the smallest molecular weights in the class, AU-15330 has proven effective in multiple oncology models including CRPC, both as a single agent and in combination with SOC.

Targeted immune checkpoint protein interventions are now clinically proven, offering immense benefits to patients. Small molecule immune checkpoint inhibitors potentially offer advantages including ease of dosing, the ability to manage immune-related adverse events (irAEs) due to their shorter pharmacokinetic exposure, and the opportunity to target more than one pathway for improving efficacy.

Utilizing the small molecule IO platform, we have developed inhibitors to several key immune checkpoint proteins. One such molecule is AUR103 – a small molecule CD47 inhibitor not expected to show toxicities such as anemia, thrombocytopenia, and leukopenia – which have been reported with several CD47 antibodies.

Since the FDA approval of imatinib in 2001, kinases have become a key target class in oncology because of their role in controlling the pathways that are transformed in cancer. Our kinase inhibitor platform utilizes a thorough understanding of the kinase inhibitor chemical space, collection of proprietary covalent and non-covalent fragments and X-ray crystallography in combination with modelling studies.

Utilizing this platform, we have discovered a number of inhibitors for various kinases that include the IRAK4 inhibitor emavusertib, which is currently undergoing global clinical development by Curis.

Synthetic peptides offer intrinsic advantages as inhibitors or activators of protein-protein interactions (PPI) for use in oncology compared with small molecules and antibodies. Our peptide drug discovery platform utilizes the crystal structure of PPIs for the rational design of peptides and further stabilization by various state-of-the art chemical modifications.

Utilizing the peptide platform, we have discovered NP-12, the first rationally designed peptide therapeutic targeting PD-1 signaling pathway.

Antibody-based therapy targeting cell surface proteins has proven to be a preferred therapeutic modality in oncology.

Our pursuit of next generation novel antibody-based therapeutics is powered by our unique antibody discovery platform. This platform synergises a proprietary large diverse human antibody library, complimentary phage and yeast surface technologies and in-house developed customizable in silico selection. We now have created a robust foundation to launching discovery programs soon for novel monoclonal antibodies, bispecific antibodies, antibody-drug conjugates, and other antibody-based therapeutics.