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entrectinib

Structure via PubChem · Public domain (PubChem)

EntityQ25323953· pop 5· linked from 500 articles

entrectinib

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Also known as NMS-E628, RXDX-101

Entrectinib, sold under the brand name Rozlytrek, is an anti-cancer medication used to treat ROS1-positive non-small cell lung cancer and NTRK fusion-positive solid tumors. It is a selective tyrosine kinase inhibitor (TKI), of the tropomyosin receptor kinases (TRK) A, B and C, C-ros oncogene 1 (ROS1) and anaplastic lymphoma kinase (ALK).

In the Vinony graph

Vinony's link graph records 500 inbound references to entrectinib, and connects out to Colorectal cancer, orphan drug and salivary gland neoplasm.

It is catalogued under topics including 4-Methylpiperazin-1-yl compounds, Benzamides and Drugs developed by Genentech.

Vinony links it to 5 Wikipedia language editions.

Chemical data

Formula
C31H34F2N6O2
Molecular weight
560.6 g/mol
IUPAC name
N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methylpiperazin-1-yl)-2-(oxan-4-ylamino)benzamide
SMILES
CN1CCN(CC1)C2=CC(=C(C=C2)C(=O)NC3=NNC4=C3C=C(C=C4)CC5=CC(=CC(=C5)F)F)NC6CCOCC6
InChIKey
HAYYBYPASCDWEQ-UHFFFAOYSA-N
XLogP
5.7
Polar surface area
85.5 Ų
H-bond donors
3
H-bond acceptors
8
Formal charge
0

via PubChem

Drug data · ChEMBL

Max clinical phase
Approved
Molecule type
Small molecule
First approval
2019
Admin. routes
oral
Indications
neoplasm, central nervous system cancer, cutaneous melanoma, non-small cell lung carcinoma

via ChEMBL · EBI

Wikidata facts

Mass
560.271
Has use
medication
Show 4 more facts
canonical SMILES
CN1CCN(CC1)C2=CC(=C(C=C2)C(=O)NC3=NNC4=C3C=C(C=C4)CC5=CC(=CC(=C5)F)F)NC6CCOCC6
medical condition treated
non-small-cell lung carcinoma
chemical formula
C₃₁H₃₄F₂N₆O₂
Sources (3)

via Wikidata · CC0

~8 min read

Encyclopedic overview

11 sections
Contents
  • Medical uses
  • Side effects
  • History
  • Mechanism of action
  • Clinical development
  • Society and culture
  • Legal status
  • Economics
  • Names
  • References
  • External links

Entrectinib, sold under the brand name Rozlytrek, is an anti-cancer medication used to treat ROS1-positive non-small cell lung cancer and NTRK fusion-positive solid tumors. It is a selective tyrosine kinase inhibitor (TKI), of the tropomyosin receptor kinases (TRK) A, B and C, C-ros oncogene 1 (ROS1) and anaplastic lymphoma kinase (ALK).

The most common side effects include tiredness, constipation, dysgeusia (taste disturbances), edema (swelling with fluid retention), dizziness, diarrhea, nausea (feeling sick), dysesthesia (unpleasant and abnormal feeling when touched), dyspnea (difficulty breathing), anemia (low red blood cell count), increased weight, increased blood creatinine (possible sign of kidney problems), pain, cognitive disorders (problems with ability to think, learn and remember), vomiting, cough, and fever.

Excerpted from Wikipedia’s “entrectinib” article, available under the CC BY-SA 4.0 licence.

Available in 5 languages

via Wikidata sitelinks · CC0

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