Purity: > 98%
Entrectinib (RXDX-101) is an oral pan-Trk, ROS1, and ALK inhibitor, with IC50 of 1.7/0.1/0.1 nM, 0.2 nM, and 1.6 nM for Trk A/B/C, ROS1, and ALK, respectively.
RXDX-101 has demonstrated potent pharmacological activity in preclinical studies and has the potential to be first-in-class against the Trk family of kinases. PXDX-101 has been well tolerated in patients with advanced solid tumors. PXDX-101 is currently in clinical trials, and is being developed by Ignyta.
1. Expert Opin Investig Drugs. 2015;24(11):1493-500. doi:
10.1517/13543784.2015.1096344. Epub 2015 Oct 12.
Entrectinib: a potent new TRK, ROS1, and ALK inhibitor.
Rolfo C(1), Ruiz R(2), Giovannetti E(3), Gil-Bazo I(4), Russo A(5), Passiglia
F(1)(5), Giallombardo M(1), Peeters M(1), Raez L(6).
(1)a Phase I - Early Clinical Trials Unit, Oncology Department , Antwerp
University Hospital and Center for Oncological Research (CORE), Antwerp
University , Edegem , Belgium.
(2)b Oncology Department , National Cancer Institute (INEN) , Lima , Peru.
(3)c Department Medical Oncology , VU University Medical Center , Amsterdam , The
(4)d Department of Oncology , Clínica Universidad de Navarra , Pamplona , Spain.
(5)e Department of Surgical, Oncological and Oral Sciences, Section of Medical
Oncology , University of Palermo , Palermo , Italy.
(6)f Thoracic Oncology Program , Memorial Cancer Institute, Memorial Health Care
System , Pembroke Pines , FL , USA.
INTRODUCTION: Receptor tyrosine kinases (RTKs) and their signaling pathways,
control normal cellular processes; however, their deregulation play important
roles in malignant transformation. In advanced non-small cell lung cancer
(NSCLC), the recognition of oncogenic activation of specific RTKs, has led to the
development of molecularly targeted agents that only benefit roughly 20% of
patients. Entrectinib is a pan-TRK, ROS1 and ALK inhibitor that has shown potent
anti-neoplastic activity and tolerability in various neoplastic conditions,
AREAS COVERED: This review outlines the pharmacokinetics, pharmacodynamics,
mechanism of action, safety, tolerability, pre-clinical studies and clinical
trials of entrectinib, a promising novel agent for the treatment of advanced
solid tumors with molecular alterations of Trk-A, B and C, ROS1 or ALK.
EXPERT OPINION: Among the several experimental drugs under clinical development,
entrectinib is emerging as an innovative and promising targeted agent. The
encouraging antitumor activity reported in the Phase 1 studies, together with the
acceptable toxicity profile, suggest that entrectinib, thanks to its peculiar
mechanism of action, could play an important role in the treatment-strategies of
multiple TRK-A, B, C, ROS1, and ALK- dependent solid tumors, including NSCLC and
colorectal cancer. That being said, further evidence for its clinical use is