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Developmental therapeutics

4813 - A Phase 1 PK/PD Study of ASN003, a novel highly selective BRAF and PI3K inhibitor, in Patients with Advanced Solid Tumors.


09 Sep 2017


Developmental therapeutics


Clinical Research


Drew Rasco


Annals of Oncology (2017) 28 (suppl_5): v122-v141. 10.1093/annonc/mdx367


D. Rasco1, R. Sullivan2, N. Lakhani3, S. Reddy4, N. Rao4, L. Denis4, A. Tolcher1, K.T. Flaherty5

Author affiliations

  • 1 Medical Oncology, South Texas Accelerated Research Therapeutics (START), 78229 - San Antonio/US
  • 2 Department Of Oncology, Massachusetts General Hospital Cancer Center, 2114 - Boston/US
  • 3 Medical Oncology, South Texas Accelerated Research Therapeutics (START), 49503 - Grand Rapids/US
  • 4 Oncology, Asana Biosciences, 08648 - Lawrenceville/US
  • 5 Termeer Center For Targeted Therapies, Massachusetts General Hospital Cancer Center, 02114 - Boston/US


Abstract 4813


RAS-RAF-MEK and PI3K-AKT-mTOR are two major pathways involved in tumor cell signaling and growth. Components of these pathways are frequently mutated in a broad range of tumors. ASN003 is a highly selective and potent (low nM IC50) inhibitor of BRAF and PI3K-α and -d (low affinity for PI3K-b). ASN003 shows strong antitumor activity in tumor models harboring BRAF and PIK3CA or PTEN mutations, and also in PDX models that are resistant to selective BRAF and MEK inhibitors.


Oral ASN003 once daily is being evaluated for safety/tolerability and preliminary efficacy in eligible patients with advanced solid tumors using an accelerated dose titration design (Part A) and enrolling cohorts of melanoma, CRC and NSCLC patients with a BRAF, PIK3CA or PTEN mutation at MTD (Part B). Eligibility criteria include HbA1c ≤ ULN or fasting glucose


Patient accrual is ongoing. To date, seven eligible patients are enrolled in dose levels ranging from 10 – 120 mg QD. ASN003 has been well tolerated. Treatment-related adverse events (TRAEs) were mild (G1) to moderate (G2). TRAEs include diarrhea (G2) (n = 1), nausea/vomiting (G1) and dry mouth/lips/skin (G1). Transient G1 elevation of glucose and insulin c-peptide levels has been noted in 1 pt. No G3/4 AEs have been observed to date. The PK profile showed excellent, systemic exposure at steady state at all doses (Cmax up to 930 ng/mL, AUC0-T up to 18998 ng.h/mL at 80 mg QD) and a half-life of > 12 hour. Dose escalation is ongoing.


ASN003 is a novel small molecule, with uniquely selective and potent inhibition of BRAF, PI3-α and -d kinases. To date, ASN003 was well tolerated at doses up to 120 mg QD and achieved good systemic exposure. Updated and detailed clinical safety/efficacy and PK/PD results will be presented.

Clinical trial identification


Legal entity responsible for the study

Asana BioSciences


Asana BioSciences


S. Reddy, N. Rao, L. Denis: Employee and Stock Ownership Asana BioSciences. A. Tolcher, K.T. Flaherty: Member of Scientific Advisory Board Asana BioSciences. All other authors have declared no conflicts of interest.

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