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Lorlatinib information


Lorlatinib
Clinical data
Trade namesLorbrena, Lorviqua
Other namesPF-6463922
AHFS/Drugs.comMonograph
MedlinePlusa619005
License data
  • US DailyMed: Lorlatinib
Pregnancy
category
  • AU: D[1]
Routes of
administration
By mouth
ATC code
  • L01ED05 (WHO)
Legal status
Legal status
  • AU: S4 (Prescription only)[1]
  • CA: ℞-only[2][3]
  • US: ℞-only[4]
  • EU: Rx-only[5]
  • 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
IUPAC name
  • (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
CAS Number
  • 1454846-35-5
PubChem CID
  • 71731823
DrugBank
  • DB12130
ChemSpider
  • 32813339
UNII
  • OSP71S83EU
KEGG
  • D11012
ChEBI
  • CHEBI:143117
CompTox Dashboard (EPA)
  • DTXSID201027944 Edit this at Wikidata
ECHA InfoCard100.245.079 Edit this at Wikidata
Chemical and physical data
FormulaC21H19FN6O2
Molar mass406.421 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • C[C@H]1Oc2cc(cnc2N)c3c(CN(C)C(=O)c4ccc(F)cc14)nn(C)c3C#N
InChI
  • 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 in the United States, Canada, and Japan, and Lorviqua in the European Union, is an anti-cancer medication used for the treatment of non-small cell lung cancer.[4] It is an orally administered inhibitor of anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (ROS1), two enzymes that play a role in the development of cancer.[6] It was developed by Pfizer.[7]

The most common adverse reactions include edema, peripheral neuropathy, weight gain, cognitive effects, fatigue, dyspnea, arthralgia, diarrhea, mood effects, hypercholesterolemia, hypertriglyceridemia, and cough.[7]

Lorlatinib was approved for medical use in the United States in November 2018,[8][9] and in the European Union in May 2019.[5]

  1. ^ a b "Lorviqua APMDS". Therapeutic Goods Administration (TGA). 26 May 2022. Archived from the original on 10 March 2024. Retrieved 10 March 2024.
  2. ^ "Lorbrena Product information". Health Canada. Archived from the original on 30 May 2022. Retrieved 29 May 2022.
  3. ^ "Summary Basis of Decision (SBD) for Lorbrena". Health Canada. 23 October 2014. Archived from the original on 31 May 2022. Retrieved 29 May 2022.
  4. ^ a b "Lorbrena- lorlatinib tablet, film coated". DailyMed. 7 September 2023. Archived from the original on 7 May 2024. Retrieved 4 June 2024.
  5. ^ a b "Lorviqua EPAR". European Medicines Agency (EMA). 6 May 2019. Archived from the original on 14 November 2021. Retrieved 4 June 2024.
  6. ^ Cite error: The named reference Nagasaka_2020 was invoked but never defined (see the help page).
  7. ^ a b Cite error: The named reference FDA 20210304 was invoked but never defined (see the help page).
  8. ^ Cite error: The named reference FDA was invoked but never defined (see the help page).
  9. ^ "Drug Approval Package: Lorbrena (lorlatinib)". U.S. Food and Drug Administration (FDA). 10 December 2018. Archived from the original on 8 November 2022. Retrieved 4 June 2024.

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Insmed mycobacterial lung disease Emicizumab-kxwh Genentech hemophilia Lorlatinib Pfizer ALK-positive, metastatic non-small cell lung cancer Brentuximab...

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common G1202R mutation that provides resistance to alectinib. Pfizer's lorlatinib was the first third-generation inhibitor and was approved in 2018 by the...

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to test the drug in patients with ROS1/NTRK/ALK gene rearrangements. Lorlatinib (also known as PF-06463922) was shown in an ongoing Phase 2 clinical trial...

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Neil Vasdev

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preliminary PET imaging of 11C and 18F isotopologues of the ROS1/ALK inhibitor lorlatinib". Nature Communications. 8 (1): 15761. Bibcode:2017NatCo...815761C. doi:10...

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