Target: Pan-HER | Indication: Gastric cancer

Introduction / Brief Description

Varlintinib, a novel, oral pan-HER inhibitor, was invented by Array and licensed to ASLAN Pharmaceuticals.  Varlintinib has shown clinical activity in both HER2-positive and EGFR-positive tumors.  In early 2015, two new trials with varlintinib were initiated:   a Phase 2 trial in Asian patients with HER2-positive metastatic breast cancer after failure of prior trastuzumab and a Phase 1 / 2 trial in combination with paclitaxel and carboplatin in Asian patients with solid tumors including HER2-positive breast cancer.  In addition, in 2014, ASLAN initiated a Phase 1b trial to evaluate safety of the combination of varlintinib with standard of car chemotherapy in patients with first line gastric cancer.  Pending appropriate results, ASLAN intends to begin a randomized Phase 2b study in gastric cancer and is exploring the use of varlintinib in other indications.

ASLAN is funding and developing varlintinib through clinical proof-of-concept. Upon achievement of proof-of-concept, ASLAN will identify a global partner for Phase 3 development and commercialization. Array will share a significant portion of the proceeds of such partnering transaction. 

Gastric cancer is a major public health problem in East Asia. Patients with locally advanced, metastatic or recurrent disease have a poor prognosis, with an overall median survival of approximately 11 months. EGFR and HER2 receptors are commonly overexpressed together in gastric cancer. Data from pivotal studies of Herceptin® (trastuzumab), indicate that the activity of this drug is limited to the subset of patients whose disease has amplified copies of the HER2 gene. We believe ASLAN001 has the potential to augment or supersede the activity of Herceptin in this population, and in the broader population of gastric cancers that co-express both EGFR and HER2 receptors.

Clinical Trials

No active trials


ASLAN001 / Cancer


Heterocyclic Compounds GRC

Process Research and Development of the Tyrosine Kinase Inhibitor Varlitinib Tosylate (ARRY-543 Ditosylate)

D. D. Hennings, et al.

ASLAN001 / Cancer


American Association for Cancer Research Annual Meeting

Selective Inhibitors of the ErbB-Family of Receptor Tyrosine Kinase

E. Wallace, Ph.D.

ASLAN001 / Cancer


American Association for Cancer Research, Chemical and Biological Aspects of Inflammation and Cancer

Pan-ErbB Inhibition by ARRY-334543 is Superior to Selective ErbB Inhibition in a Preclinical Model that Signals Through Multiple ErbB Receptors

R. Blackwell, et al.