Pralsetinib
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Names | |
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Trade names | Gavreto |
Other names | BLU-667 |
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Clinical data | |
Drug class | Tyrosine kinase inhibitor[1] |
Main uses | Non-small cell lung cancer (NSCLC), thyroid cancer[1] |
Side effects | Constipation, high blood pressure, tiredness, muscle pain, low blood cells, liver problems, low calcium[1] |
Routes of use | By mouth |
Typical dose | 400 mg OD[1] |
External links | |
AHFS/Drugs.com | Monograph |
MedlinePlus | a620057 |
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License data |
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Legal status | |
Chemical and physical data | |
Formula | C27H32FN9O2 |
Molar mass | 533.612 g·mol−1 |
3D model (JSmol) | |
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Pralsetinib, sold under the brand name Gavreto, is a medication used to treat non-small cell lung cancer (NSCLC) and thyroid cancer.[1] It is used in advanced cases which are RET fusion-positive.[1] It is taken by mouth.[1]
Common side effects include constipation, high blood pressure, tiredness, muscle pain, low blood cells, liver problems, and low calcium.[1] Other side effects may include pneumonitis, bleeding, tumor lysis syndrome, and poor wound healing.[1] Use in pregnancy may harm the baby.[1] It is a tyrosine kinase inhibitor.[1]
Pralsetinib was approved for medical use in the United States in 2020.[1] In the United States it costs about 20,100 USD per month.[2] It is not approved for use in the United Kingdom as of 2021.[3]
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.[4][5]
Dosage
It is generally taken at a dose of 400 mg once daily.[1]
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.[4][5] Identification of RET gene alterations was prospectively determined in local laboratories using either next generation sequencing, fluorescence in situ hybridization, or other tests.[4] The main efficacy outcome measures were overall response rate (ORR) and response duration determined by a blinded independent review committee using RECIST 1.1.[4] The trial was conducted at sites in the United States, Europe and Asia.[5]
Efficacy for RET fusion-positive NSCLC was evaluated in 87 participants previously treated with platinum chemotherapy.[4] The ORR was 57% (95% CI: 46%, 68%); 80% of responding participants had responses lasting 6 months or longer.[4] Efficacy was also evaluated in 27 participants who never received systemic treatment.[4] The ORR for these participants was 70% (95% CI: 50%, 86%); 58% of responding participants had responses lasting 6 months or longer.[4]
The US Food and Drug Administration (FDA) granted the application for pralsetinib priority review, orphan drug, and breakthrough therapy designations[4]and granted approval of Gavreto to Blueprint Medicines.[4]
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).[7] The applicant for this medicinal product is Roche Registration GmbH.[7]
References
- ↑ 1.00 1.01 1.02 1.03 1.04 1.05 1.06 1.07 1.08 1.09 1.10 1.11 1.12 1.13 "Gavreto- pralsetinib capsule". DailyMed. 9 September 2020. Archived from the original on 28 November 2020. Retrieved 24 September 2020.
- ↑ "Gavreto Prices, Coupons & Patient Assistance Programs". Drugs.com. Retrieved 29 October 2021.
- ↑ "Pralsetinib". SPS - Specialist Pharmacy Service. 4 July 2020. Archived from the original on 29 October 2021. Retrieved 29 October 2021.
- ↑ 4.0 4.1 4.2 4.3 4.4 4.5 4.6 4.7 4.8 4.9 "FDA approves pralsetinib for lung cancer with RET gene fusions". U.S. Food and Drug Administration (FDA). 4 September 2020. Archived from the original on 9 September 2020. Retrieved 8 September 2020.
This article incorporates text from this source, which is in the public domain.
- ↑ 5.0 5.1 5.2 "Drug Trial Snapshot: Gavreto". U.S. Food and Drug Administration. 4 September 2020. Archived from the original on 25 October 2020. Retrieved 16 September 2020.
This article incorporates text from this source, which is in the public domain.
- ↑ Sun, Shi-Yong; Su, Chunxia (30 August 2022). Challenges and Opportunities of TKIs in the Treatment of NSCLC Patients With Uncommon Mutations. Frontiers Media SA. p. 9. ISBN 978-2-88976-866-0. Retrieved 25 November 2023.
- ↑ 7.0 7.1 "Gavreto: Pending EC decision". European Medicines Agency. 17 September 2021. Archived from the original on 17 September 2021. Retrieved 17 September 2021. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
External links
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Identifiers: |
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- "Pralsetinib". NCI Drug Dictionary. National Cancer Institute. Archived from the original on 14 July 2020. Retrieved 24 September 2021.
- Clinical trial number NCT03037385 for "Phase 1/2 Study of the Highly-selective RET Inhibitor, Pralsetinib (BLU-667), in Patients With Thyroid Cancer, Non-Small Cell Lung Cancer, and Other Advanced Solid Tumors (ARROW)" at ClinicalTrials.gov
- "Understanding Metastatic RET Fusion-Positive Non-Small Cell Lung Cancer (NSCLC)" (PDF). Archived (PDF) from the original on 13 December 2020. Retrieved 24 September 2021.
- "Understanding Metastatic RET-Driven Thyroid Cancers" (PDF). Archived (PDF) from the original on 19 September 2020. Retrieved 24 September 2021.
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