Pralsetinib Explained

Width:300
Tradename:Gavreto
Dailymedid:Pralsetinib
Pregnancy Au:D
Pregnancy Au Comment:[1]
Routes Of Administration:By mouth
Class:Tyrosine kinase inhibitor
Atc Prefix:L01
Atc Suffix:EX23
Legal Au:S4
Legal Au Comment:[2] [3] [4] [5]
Legal Ca:Rx-only
Legal Ca Comment:[6]
Legal Us:Rx-only
Legal Us Comment:[7]
Legal Eu:Rx-only
Legal Eu Comment:[8] [9]
Cas Number:2097132-94-8
Pubchem:129073603
Drugbank:DB15822
Chemspiderid:71060332
Unii:1WPE73O1WV
Kegg:D11712
Chembl:4297597
Synonyms:BLU-667
Iupac Name:N-[(1S)-1-[6-(4-fluoropyrazol-1-yl)pyridin-3-yl]ethyl]-1-methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]cyclohexane-1-carboxamide
C:27
H:32
F:1
N:9
O:2
Smiles:CC1=CC(=NN1)NC2=NC(=NC(=C2)C)C3CCC(CC3)(C(=O)NC(C)C4=CN=C(C=C4)N5C=C(C=N5)F)OC
Stdinchi:1S/C27H32FN9O2/c1-16-11-22(33-23-12-17(2)35-36-23)34-25(31-16)19-7-9-27(39-4,10-8-19)26(38)32-18(3)20-5-6-24(29-13-20)37-15-21(28)14-30-37/h5-6,11-15,18-19H,7-10H2,1-4H3,(H,32,38)(H2,31,33,34,35,36)/t18-,19?,27?/m0/s1
Stdinchikey:GBLBJPZSROAGMF-SIYOEGHHSA-N

Pralsetinib, sold under the brand name Gavreto, is a medication approved[10] for RET mutation-positive medullary thyroid cancer (MTC)[11] and RET fusion-positive differentiated thyroid cancer (DTC) refractory to radioactive iodine (RAI) therapy. Pralsetinib is a tyrosine kinase inhibitor. It is taken by mouth.

The most common adverse reactions include increased aspartate aminotransferase (AST), decreased hemoglobin, decreased lymphocytes, decreased neutrophils, increased alanine aminotransferase (ALT), increased creatinine, increased alkaline phosphatase, fatigue, constipation, musculoskeletal pain, decreased calcium, hypertension, decreased sodium, decreased phosphate, and decreased platelets.

Pralsetinib was approved for medical use in the United States in September 2020,[12] [13] [14] and in the European Union in November 2021.

Medical uses

Pralsetinib is indicated for the treatment of adults with metastatic RET fusion-positive non-small cell lung cancer (NSCLC) as detected by an FDA approved test.[15] [16]

History

Efficacy was investigated in a multicenter, open-label, multi-cohort clinical trial (ARROW, NCT03037385) with 220 participants aged 26-87 whose tumors had RET alterations. Identification of RET gene alterations was prospectively determined in local laboratories using either next generation sequencing, fluorescence in situ hybridization, or other tests. The main efficacy outcome measures were overall response rate (ORR) and response duration determined by a blinded independent review committee using RECIST 1.1. The trial was conducted at sites in the United States, Europe and Asia.

Efficacy for RET fusion-positive NSCLC was evaluated in 87 participants previously treated with platinum chemotherapy. The ORR was 57% (95% CI: 46%, 68%); 80% of responding participants had responses lasting 6 months or longer. Efficacy was also evaluated in 27 participants who never received systemic treatment. The ORR for these participants was 70% (95% CI: 50%, 86%); 58% of responding participants had responses lasting 6 months or longer.

The US Food and Drug Administration (FDA) granted the application for pralsetinib priority review, orphan drug, and breakthrough therapy designationsand granted approval of Gavreto to Blueprint Medicines.

Society and culture

Legal status

On 16 September 2021, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a conditional marketing authorization for the medicinal product Gavreto, intended for the treatment of people with rearranged during transfection (RET)-fusion positive non-small cell lung cancer (NSCLC). The applicant for this medicinal product is Roche Registration GmbH.[17] Pralsetinib was approved for medical use in the European Union in November 2021.

External links

Notes and References

  1. Web site: Gavreto . Therapeutic Goods Administration (TGA) . 6 April 2023 . 7 April 2023 . 8 April 2023 . https://web.archive.org/web/20230408034301/https://www.tga.gov.au/resources/auspmd/gavreto . live .
  2. Web site: Gavreto pralsetinib 100 mg hard capsule bottle (380812) . Therapeutic Goods Administration (TGA) . 30 March 2023 . 7 April 2023 . 8 April 2023 . https://web.archive.org/web/20230408034432/https://www.tga.gov.au/resources/artg/380812 . live .
  3. Web site: Gavreto (Roche Products Pty Ltd) . Therapeutic Goods Administration (TGA) . 26 April 2023 . 28 April 2023.
  4. Web site: Gavreto (Roche Products Pty Ltd) . Therapeutic Goods Administration (TGA) . 26 April 2023 . 28 April 2023.
  5. https://www.tga.gov.au/resources/auspar/auspar-gavreto-0
  6. Web site: Summary Basis of Decision (SBD) for Gavreto . Health Canada . 23 October 2014 . 29 May 2022 . 29 May 2022 . https://web.archive.org/web/20220529200533/https://hpr-rps.hres.ca/reg-content/summary-basis-decision-detailTwo.php?linkID=SBD00559&lang=en . live .
  7. Web site: Gavreto- pralsetinib capsule . DailyMed . 9 September 2020 . 24 September 2020 . 28 November 2020 . https://web.archive.org/web/20201128145353/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=beb226ab-f684-42de-93a4-edb2263ddb11 . live .
  8. Web site: Gavreto EPAR . European Medicines Agency (EMA) . 14 September 2021 . 9 December 2021 . 10 December 2021 . https://web.archive.org/web/20211210085329/https://www.ema.europa.eu/en/medicines/human/EPAR/gavreto . live .
  9. Web site: Gavreto Product information . Union Register of medicinal products . 3 March 2023 . 5 March 2023 . https://web.archive.org/web/20230305040638/https://ec.europa.eu/health/documents/community-register/html/h1555.htm . live .
  10. Web site: Center for Drug Evaluation and Research . 2021-06-11 . FDA approves pralsetinib for RET-altered thyroid cancers . U.S. Food and Drug Administration . en . 9 January 2023 . 9 January 2023 . https://web.archive.org/web/20230109101839/https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-pralsetinib-ret-altered-thyroid-cancers . live .
  11. Nervo A, Retta F, Ragni A, Piovesan A, Gallo M, Arvat E . Management of Progressive Radioiodine-Refractory Thyroid Carcinoma: Current Perspective . Cancer Management and Research . 14 . 3047–3062 . 2022 . 36275786 . 9584766 . 10.2147/CMAR.S340967 . free .
  12. Blueprint Medicines . Blueprint Medicines Announces FDA Approval of Gavreto (pralsetinib) for the Treatment of Adults with Metastatic RET Fusion-Positive Non-Small Cell Lung Cancer . PR Newswire . 4 September 2020 . 8 September 2020 . 9 September 2020 . https://web.archive.org/web/20200909051400/https://www.prnewswire.com/news-releases/blueprint-medicines-announces-fda-approval-of-gavreto-pralsetinib-for-the-treatment-of-adults-with-metastatic-ret-fusion-positive-non-small-cell-lung-cancer-301124707.html . live .
  13. Roche announces FDA approval of Gavreto (pralsetinib) for the treatment of adults with metastatic RET fusion-positive non-small cell lung cancer . Roche . 7 September 2020 . 8 September 2020 . 9 September 2020 . https://web.archive.org/web/20200909051453/https://www.roche.com/media/releases/med-cor-2020-09-07.htm . live .
  14. Markham A . Pralsetinib: First Approval . Drugs . 80 . 17 . 1865–1870 . November 2020 . 33136236 . 10.1007/s40265-020-01427-4 . 226223522 .
  15. Web site: FDA approves pralsetinib for lung cancer with RET gene fusions . U.S. Food and Drug Administration (FDA) . 4 September 2020 . 8 September 2020 . 9 September 2020 . https://web.archive.org/web/20200909051417/https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-pralsetinib-lung-cancer-ret-gene-fusions . live .
  16. Web site: Drug Trial Snapshot: Gavreto . U.S. Food and Drug Administration . 4 September 2020 . 16 September 2020 . 25 October 2020 . https://web.archive.org/web/20201025213703/https://www.fda.gov/drugs/drug-approvals-and-databases/drug-trial-snapshot-gavreto . live .
  17. Web site: Gavreto: Pending EC decision . European Medicines Agency . 17 September 2021 . 17 September 2021 . 17 September 2021 . https://web.archive.org/web/20210917190507/https://www.ema.europa.eu/en/medicines/human/summaries-opinion/gavreto . live . Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Pralsetinib".

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