Mr. Ibrahem/Entrectinib
Clinical data
Trade namesRozlytrek
Other namesRXDX-101, NMS-E628
AHFS/Drugs.comMonograph
MedlinePlusa619049
License data
Pregnancy
category
Routes of
administration
By mouth
Drug classTyrosine kinase inhibitor[2]
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
Chemical and physical data
FormulaC31H34F2N6O2
Molar mass560.650 g·mol−1
3D model (JSmol)
  • CN1CCN(CC1)C2=CC(=C(C=C2)C(=O)NC3=NNC4=C3C=C(C=C4)CC5=CC(=CC(=C5)F)F)NC6CCOCC6
  • 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 a medication used to treat non-small cell lung cancer (NSCLC) which are ROS1-positive or solid tumors that are NTRK fusion-positive.[4] It is taken by mouth.[4]

Common side effects include tiredness, constipation, change in taste, swelling due to fluid retention, dizziness, diarrhea, nausea, numbness, difficulty breathing, increased weight, cough, fever, thinking problems, and vision problems.[4] Other side effects include heart failure, bone fractures, liver problems, high uric acid, and QT prolongation.[4] Use in pregnancy may harm the baby.[4] It is a tyrosine kinase inhibitor (TKI), of the tropomyosin receptor kinases (TRK) A, B and C, C-ros oncogene 1 (ROS1), and anaplastic lymphoma kinase (ALK).[2]

Entrectinib was approved for medical use in the United States in 2019, and Australia and Europe in 2020.[4][1][5] In the United Kingdom a month of treatment costs the NHS about £5,200 as of 2021.[6] This amount in the United States costs about 16,800 USD.[7]

References edit

  1. ^ a b c "Rozlytrek Australian prescription medicine decision summary". Therapeutic Goods Administration (TGA). 25 May 2020. Archived from the original on 8 October 2020. Retrieved 16 August 2020.
  2. ^ a b "Entrectinib Monograph for Professionals". Drugs.com. Archived from the original on 13 October 2020. Retrieved 15 December 2021.
  3. ^ "Rozlytrek 100 mg hard capsules - Summary of Product Characteristics (SmPC)". (emc). Archived from the original on 9 October 2020. Retrieved 11 September 2020.
  4. ^ a b c d e f g h i j "Rozlytrek- entrectinib capsule". DailyMed. 8 June 2020. Archived from the original on 27 February 2021. Retrieved 16 August 2020.
  5. ^ a b "Rozlytrek EPAR". European Medicines Agency (EMA). 26 May 2020. Archived from the original on 28 October 2020. Retrieved 11 September 2020. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  6. ^ BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 1024. ISBN 978-0857114105.
  7. ^ "Entrectinib Prices, Coupons & Savings Tips - GoodRx". GoodRx. Retrieved 15 December 2021.