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1108743-60-7

1108743-60-7 Structure

1108743-60-7 Structure
IdentificationBack Directory
[Name]

Entrectinib
[CAS]

1108743-60-7
[Synonyms]

CS-1589
RXDX-101
NMS-E628
Entrectinib
entrecitinib
Entrectinib(RXDX-101)
Entrectinib(NMS-E628)
Entrectinib,NMS-E628,RXDX-101
NMS E628; RXDX-101;NMSE628; RXDX 101;NMS-E628; RXDX101
RXDX101; RXDX 101; RXDX-101; NMS E628; NMSE628; NMS-E628; ENTRECTINIB
N-(5-(3,5-difluorobenzyl)-1H-indazol-3-yl)-4-(4-methylpiperazin-1-yl)-2-(tetrahydro-2H-pyran-4-ylamino)benzamide
N-[5-[(3,5-Difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methyl-1-piperazinyl)-2-[(tetrahydro-2H-pyran-4-yl)amino]benzamide
Benzamide, N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methyl-1-piperazinyl)-2-[(tetrahydro-2H-pyran-4-yl)amino]-
[Molecular Formula]

C31H34F2N6O2
[MOL File]

1108743-60-7.mol
[Molecular Weight]

560.64
Questions And AnswerBack Directory
[Description]

Entrectinib is used to treat metastatic (lung cancer that has already spread) non-small cell lung cancer (NSCLC) that is caused by a gene called ROS1. This medicine is also used to treat solid tumors (cancer) that are caused by certain abnormal NTRK genes and have spread or if surgery to remove the cancer is likely to cause severe complications, and there is no acceptable treatment option or the cancer grew or spread on other treatments.
[Effect and benefit]

Entrectinib belongs to the group of medicines called antineoplastics (cancer medicines). It works by interfering with the growth of cancer cells, which are eventually destroyed.
[Mechanism of action]

An inhibitor of tropomyosin receptor tyrosine kinases (TRKs) TRKA, TRKB, and TRKC (encoded by the neurotrophic tyrosine receptor kinase [NTRK] genes NTRK1, NTRK2, and NTRK3, respectively), proto-oncogene tyrosine-protein kinase ROS1 (ROS1), and anaplastic lymphoma kinase (ALK); also, inhibits JAK2 and TNK2. Major active metabolite of entrectinib, M5, showed similar in vitro activity against TRK, ROS1, and ALK. Fusion proteins that include TRK, ROS1, or ALK kinase domains can drive tumorigenic potential through hyperactivation of downstream signaling pathways, leading to unconstrained cell proliferation.
[Safety]

Entrectinib exhibits hepatic metabolism through cytochrome P450 (CYP) 3A and therefore interacts with moderate-strong CYP3A inhibitors and inducers. In addition, due to its effects on the QTcF interval, use of entrectinib should be avoided with other drugs known to prolong the QT/QTc interval.
[Pharmacology]

Entrectinib, is a weak P-gp substrate that can sustain CNS exposure based on our novel in vitro and in vivo experiments. This is consistent with the observed preclinical and clinical efficacy of entrectinib in neurotrophic tropomyosin receptor kinase (NTRK) and ROS1 fusion-positive CNS tumors and secondary CNS metastases.
Chemical PropertiesBack Directory
[Boiling point ]

717.5±60.0 °C(Predicted)
[density ]

1.340±0.06 g/cm3(Predicted)
[pka]

12.01±0.43(Predicted)
Hazard InformationBack Directory
[Clinical Use]

Entrectinib demonstrated potent antitumor effects in tumor cell lines and patient-derived xenograft (PDX) tumor models in preclinical studies. Furthermore, entrectinib can cross the blood–brain barrier (BBB) to impact primary brain tumors and brain metastases in patients with NTRK1/ NTRK2/NTRK3, ROS1, and ALK fusion-driven cancers.
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