Our Pipeline

Methylenetetrahydrofolate dehydrogenase 2

MTHFD2 is a mitochondrial enzyme involved in the folate-mediated one-carbon metabolism pathway. It plays a crucial role in controlling the fate and function of Th17 cells, and its inhibition promotes a Treg cell-like phenotype.

MTHFD2 deficiency has been shown to reduce disease severity in multiple in vivo inflammatory disease models. Pharmacological inhibition of MTHFD2 has the potential to treat various inflammatory conditions with an improved safety profile compared to JAK1 inhibitors.

We have applied our AI-driven drug discovery platforms, Makya and Spaya, to identify novel, potent, and selective MTHFD2 inhibitors. IKT525, a representative molecule from our lead series, is a potent (IC50 < 5nM), selective (>1000X over MTHFD1), and potential first-in-class MTHFD2 inhibitor with desirable drug-like properties. Preclinical candidate nomination is expected by 2025.

Amylin Receptor

Amylin receptor agonists offer significant potential for addressing unmet medical needs in cardiometabolic disorders, including obesity, diabetes, and metabolic dysfunction-associated steatotic hepatitis (MASH). While therapies like GLP-1 receptor agonists (e.g., semaglutide) and the peptide Amylin analogue pramlintide have shown efficacy, their impact is often limited by high costs, limited accessibility, and side effects.

Novel small molecule agonists of the Amylin receptor—developed for oral administration—could overcome these barriers, providing scalable, effective, and accessible treatments for the growing obesity epidemic and its related comorbidities. However, the structural and biological complexity of the Amylin receptor has historically hindered the discovery of low-molecular-weight modulators.

To address this challenge, we have partnered with Cube Biotech to co-develop novel Amylin receptor agonists. Cube’s cutting-edge protein stabilization technology preserves the natural conformation of membrane proteins, enabling access to biologically active drug targets for testing. Combined with our AI-driven drug discovery platform, this collaboration aims to accelerate the development of breakthrough small molecule therapies targeting the Amylin receptor.

Protein Kinase Membrane associated Tyrosine/Threonine 1

PKMYT1 (Protein Kinase, Membrane Associated Tyrosine/Threonine 1) is a member of the serine/threonine protein kinase family. PKMYT1 is important in regulating the cell cycle through inactivating the cyclin-dependent kinase 1 CDK1.

Inhibiting PKMYT1 disrupts the G2/M checkpoint leading to premature mitosis and catastrophic DNA damage in cells harboring synthetic lethal genomic alterations such as CCNE1. Amplification of CCNE1 (cyclin E) is prevalent in multiple tumor types, ovarian cancer, uterine and gastro- oesophageal. Cancers with CCNE1-amplification are often resistant to standard of care treatment and represent an unmet clinical need.

Pharmacological inhibition PKMYT1 in high CCNE1–expressing tumor cells is synthetic lethal and leads to DNA damage through premature mitotic entry. PKMYT1 inhibition is a promising therapeutic strategy for CCNE1-amplified cancers and other genetically altered cancers such as background FBXW7.

We have applied our AI-driven drug discovery platforms, Makya and Spaya, to identify novel, potent and selective PKMYT1 inhibitors. We have generated in less than 3 months a  novel hit series with 30 nM potency and desirable drug-like properties. 

SKP2-CKS1 PPI inhibitors

The cyclin‐dependent kinase inhibitor p27 is a critical cell cycle regulator frequently altered in human cancer.  Protein p27 binds and inhibits cyclin-CDK to arrest the cell cycle.  The cellular level of p27 is controlled by ubiquitin‐dependent degradation mediated by the E3 ligase SCF-Skp2 and its accessory protein - Cks1, which promote proliferation largely by inducing the degradation of the CDK inhibitor p27. Overexpression of Skp2 in human cancers correlates with poor prognosis, and deregulation of SCF-Skp2-Cks1 promotes tumorigenesis in animal models.

Designing Skp2- CKS1 specific Protein-Protein interaction (PPI) inhibitors is a novel strategy to treat cancers dependent on the Skp2-p27 axis.

We are applying our AI-driven drug discovery platforms, Makya and Spaya and our PPI cellular technology MTBench to identify novel SKP2-CKS1 inhibitors. We have identified a very specific binding interface between the 2 proteins in which our AI is generating novel molecules.