A Phase Ib, Open-label, Multi-center, Dose-escalation and Expansion Study of an Orally Administered Combination of BKM120 Plus MEK162 in Adult Patients With Selected Advanced Solid Tumors

Trial ID # NCT01363232
Phase I
Drug Class Signaling Pathway Inhibitors: PI3K-AKT-mTOR/pan-PI3K
Drug Name Buparlisib
Alternate Drug Names BKM120, NVP-BKM120, AN2025
Drugs in Trial Binimetinib, Buparlisib
Eligible Participant

Advanced solid tumors with RAS or RAF alterations

Patients Enrolled

89, median 3 prior therapies (1-12); 19 ovarian

Therapy Setting


Study Design

Open-Label, Non-randomized


ORR, DCR, PFS, RP2D, evaluated per RECIST


KRAS, NRAS, BRAF alterations


RP2D: 80 mg buparlisib qd+45 mg binimetinib bid

ovarian patients at RP2D:
ORR: 27.8% (5PR, n=18; 2 KRAS MUT, 1 NRAS MUT, 2 BRAF MUT)
DCR: 61.1% (5PR, 6SD, n=18)
PFS: 3.7 months

Clinically Significant Adverse Events

Serious AE:
Grade 3-4 AE: maculopapular rash (12.4%)


Buparlisib+binimetinib shows encouraging efficacy in RAS/RAF MUT ovarian cancer patients, but with significant toxicity


Bardia A et al. Phase Ib Study of Combination Therapy with MEK Inhibitor Binimetinib and Phosphatidylinositol 3-Kinase Inhibitor Buparlisib in Patients with Advanced Solid Tumors with RAS/RAF Alterations. Oncologist (2020) 25(1):e160-e169

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