Pursuit of Targeted Therapies

Pipeline

Backed by well-validated targets and our innovative data and screening platforms, we focus on developing therapies that promise a better future for patients worldwide. 

PROGRAM

INDICATION

DISCOVERY

IND ENABLING

PHASE 1/2

PARTNERS

TYK2
ARTS-011

Autoimmune

ARTS-011 is a highly selective, potent and orally available TYK2 inhibitor with suitable pharmaceutical properties to be a potential therapy for inflammatory disorders. It exhibits excellent selectivity against other JAK family kinases and demonstrates great DMPK properties and safety profiles. ARTS-011 has completed Phase 1 clinical trial in healthy volunteers in China.

CDK2
ARTS-021

Oncology

ARTS-021 is a highly potent and selective inhibitor of CDK2, a key enzyme involved in cell cycle regulation. In preclinical studies, ARTS-021 demonstrated ability to selectively inhibit the growth of tumors with CCNE1 amplification. It can also overcome the resistance that ER+/HER2- breast cancer cells develop against CDK4/6 inhibitors. Partnering with Avenzo Therapeutics, ARTS-021 (AVZO-021) is being studied in a Phase 1 study in the U.S. for the treatment of advanced solid tumors and will be advanced globally.

Synthetic lethal target

Oncology

Isoform-selective kinase inhibitor

Oncology

ARTS-023 is an orally bioavailable CDK4 inhibitor with high selectivity over CDK6. In enzymatic assays, ARTS-023 potently inhibits the CDK4/Cyclin D1 complex, with an IC₅₀ in the sub-nanomolar range, demonstrating strong selectivity against CDK6 and other CDKs tested. At
low nanomolar concentrations, ARTS-023 effectively inhibits Rb phosphorylation and blocks the G1/S cell cycle transition, leading to growth arrest in ER-positive breast cancer cell lines. ARTS-023 has also shown robust anti-tumor activity as a single agent in multiple ER-positive breast cancer xenograft models. With the potential to become a best-in-class oncology therapy for patients with HR+/HER2- breast cancer, ARTS-023 (AVZO-023), in partnership with Avenzo Therapeutics, is currently being evaluated in a Phase 1 study in the U.S. for the treatment of advanced solid tumors, with plans for global development.

EGFR L858R allosteric inhibitor

Oncology

Allorion’s premier allosteric inhibitor program is targeting an exquisitely selective and potent inhibitor of L858R and other activating mutations of EGFR. Binding to a unique cavity, distinct from the ATP pocket, lead candidates have the potential to enhance the activity of existing ATP-competitive inhibitors, when dosed in combination, to more effectively address EGFR resistance mutations or even prevent their emergence, thereby providing increased benefit for patients.