Entrectinib

Entrectinib
Clinical data
Trade namesRozlytrek
Other namesRXDX-101, NMS-E628
AHFS/Drugs.comMonograph
MedlinePlusa619049
License data
Pregnancy
category
Routes of
administration		By mouth
Drug classAntineoplastic agent
ATC code
Legal status
Legal status
Identifiers
  • N-[5-(3,5-Difluorobenzyl)-1H-indazol-3-yl]-4-(4-methyl-1-piperazinyl)-2-(tetrahydro-2H-pyran-4-ylamino)benzamide
CAS Number
PubChem CID
PubChem SID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC31H34F2N6O2
Molar mass560.650 g·mol−1
3D model (JSmol)
  • CN1CCN(c2ccc(C(=O)Nc3n[nH]c4ccc(Cc5cc(F)cc(F)c5)cc34)c(NC3CCOCC3)c2)CC1
  • InChI=1S/C31H34F2N6O2/c1-38-8-10-39(11-9-38)25-3-4-26(29(19-25)34-24-6-12-41-13-7-24)31(40)35-30-27-17-20(2-5-28(27)36-37-30)14-21-15-22(32)18-23(33)16-21/h2-5,15-19,24,34H,6-14H2,1H3,(H2,35,36,37,40)
  • Key:HAYYBYPASCDWEQ-UHFFFAOYSA-N

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.[5] 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).[5]

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.[6][8]

It was approved for medical use in the United States in August 2019,[8][9][10] in Australia in May 2020,[1] and in the European Union in July 2020.[6]

  1. ^ a b c "Rozlytrek Australian prescription medicine decision summary". Therapeutic Goods Administration (TGA). 25 May 2020. Retrieved 16 August 2020.
  2. ^ "Rozlytrek Product information". Health Canada. Retrieved 29 May 2022.
  3. ^ "Summary Basis of Decision (SBD) for Rozlytrek". Health Canada. 23 October 2014. Retrieved 29 May 2022.
  4. ^ "Rozlytrek 100 mg hard capsules - Summary of Product Characteristics (SmPC)". (emc). Retrieved 11 September 2020.
  5. ^ a b c Cite error: The named reference Rozlytrek FDA label was invoked but never defined (see the help page).
  6. ^ a b c Cite error: The named reference Rozlytrek EPAR was invoked but never defined (see the help page).
  7. ^ "Rozlytrek Product information". Union Register of medicinal products. Retrieved 3 March 2023.
  8. ^ a b "FDA approves third oncology drug that targets a key genetic driver of cancer, rather than a specific type of tumor". U.S. Food and Drug Administration (FDA) (Press release). 15 August 2019. Archived from the original on 14 September 2019. Retrieved 23 November 2019. Public Domain This article incorporates text from this source, which is in the public domain.
  9. ^ "FDA Approves Genentech's Rozlytrek (entrectinib) for People With ROS1-Positive, Metastatic Non-Small Cell Lung Cancer and NTRK Gene Fusion-Positive Solid Tumors". Genentech (Press release). Retrieved 16 August 2019.
  10. ^ "Drug Approval Package: Rozlytrek". U.S. Food and Drug Administration (FDA). 16 September 2019. Retrieved 23 November 2019.