User:Mr. Ibrahem/Lorlatinib

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Mr. Ibrahem/Lorlatinib
Clinical data
Trade namesLorbrena, Lorviqua
Other namesPF-6463922
AHFS/Drugs.comMonograph
MedlinePlusa619005
License data
Pregnancy
category
  • AU: D
Routes of
administration		By mouth
Drug classTyrosine kinase inhibitor[1]
Legal status
Legal status
  • AU: S4 (Prescription only)
  • US: ℞-only
  • EU: Rx-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability81%
Protein binding66%
MetabolismMainly CYP3A4 and UGT1A4
Elimination half-life24 hrs (single dose)
Excretion48% urine (<1% unchanged), 41% faeces (9% unchanged)
Identifiers
  • (10R)-7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-4,8-methenopyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile
Chemical and physical data
FormulaC21H19FN6O2
Molar mass406.421 g·mol−1
3D model (JSmol)
  • C[C@H]1Oc2cc(cnc2N)c3c(CN(C)C(=O)c4ccc(F)cc14)nn(C)c3C#N
  • InChI=1S/C21H19FN6O2/c1-11-15-7-13(22)4-5-14(15)21(29)27(2)10-16-19(17(8-23)28(3)26-16)12-6-18(30-11)20(24)25-9-12/h4-7,9,11H,10H2,1-3H3,(H2,24,25)/t11-/m1/s1
  • Key:IIXWYSCJSQVBQM-LLVKDONJSA-N

Lorlatinib, sold under the brand name Lorbrena and Lorviqua, is a medication used to treat non-small cell lung cancer (NSCLC).[1] Specifically it is used in anaplastic lymphoma kinase (ALK) positive cases that have failed other treatments.[1] It is taken by mouth.[1]

Common side effects are high cholesterol, high triglycerides, swelling, peripheral neuropathy, problems with memory, tiredness, weight gain, and joint pain.[2] Other side effects may include liver problems, seizures, hallucinations, pneumonitis, and AV block.[1] Use in pregnancy may harm the baby.[1] It is a tyrosine kinase inhibitor of ALK and ROS1.[1]

Lorlatinib was approved for medical use in the United States in 2018 and Europe in 2019.[1][2] In the United Kingdom it costs the NHS about £5,300 a month as of 2021.[3] This amount in the United States is about 18,500 USD.[4]

References[edit]

  1. ^ a b c d e f g h i j "Lorlatinib Monograph for Professionals". Drugs.com. Archived from the original on 4 March 2021. Retrieved 24 November 2021.
  2. ^ a b c "Lorviqua". Archived from the original on 14 November 2021. Retrieved 24 November 2021.
  3. ^ BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 1033. ISBN 978-0857114105.
  4. ^ "Lorbrena Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 26 January 2021. Retrieved 24 November 2021.
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