capivasertib
{{Use American English|date=November 2023}}
{{Use dmy dates|date=November 2023}}
{{cs1 config |name-list-style=vanc |display-authors=6}}
{{Infobox drug
| image = Capivasertib.svg
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| pronounce =
| tradename = Truqap
| Drugs.com = {{drugs.com|drugs.com|monograph/capivasertib}}
| MedlinePlus = a623056
| DailyMedID = Capivasertib
| pregnancy_AU = D
| pregnancy_AU_comment = {{cite web | title=Truqap (capivasertib) | website=Therapeutic Goods Administration (TGA) | date=17 June 2024 | url=https://www.tga.gov.au/resources/auspmd/truqap-capivasertib | access-date=7 July 2024}}
| pregnancy_category=
| routes_of_administration = By mouth
| class = Threonine kinase inhibitor
| ATC_prefix = L01
| ATC_suffix = EX27
| ATC_supplemental =
| legal_AU = S4
| legal_AU_comment = {{cite web | title=Truqap (AstraZeneca Pty Ltd) | website=Therapeutic Goods Administration (TGA) | date=31 May 2024 | url=https://www.tga.gov.au/resources/prescription-medicines-registrations/truqap-astrazeneca-pty-ltd | access-date=17 June 2024 | archive-date=17 June 2024 | archive-url=https://web.archive.org/web/20240617031755/https://www.tga.gov.au/resources/prescription-medicines-registrations/truqap-astrazeneca-pty-ltd | url-status=live }}
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| legal_CA = Rx-only
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| legal_US = Rx-only
| legal_EU = Rx-only
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| CAS_number = 1143532-39-1
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| PubChem = 25227436
| IUPHAR_ligand =
| DrugBank = DB12218
| ChemSpiderID = 28189073
| UNII = WFR23M21IE
| KEGG = D11371
| ChEBI = 229222
| ChEMBL = 2325741
| NIAID_ChemDB =
| PDB_ligand = 0XZ
| synonyms = AZD-5363, AZD5363
| IUPAC_name = 4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide
| C=21|H=25|Cl=1|N=6|O=2
| SMILES = NC1(CCN(CC1)C1=C2C=CNC2=NC=N1)C(=O)N[C@@H](CCO)C1=CC=C(Cl)C=C1
| StdInChI = 1S/C21H25ClN6O2/c22-15-3-1-14(2-4-15)17(6-12-29)27-20(30)21(23)7-10-28(11-8-21)19-16-5-9-24-18(16)25-13-26-19/h1-5,9,13,17,29H,6-8,10-12,23H2,(H,27,30)(H,24,25,26)/t17-/m0/s1
| StdInChI_comment =
| StdInChIKey = JDUBGYFRJFOXQC-KRWDZBQOSA-N
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Capivasertib, sold under the brand name Truqap, is an anti-cancer medication used for the treatment of breast cancer.{{cite journal | doi = 10.1056/NEJMoa2214131 | title = Capivasertib in Hormone Receptor–Positive Advanced Breast Cancer | date = June 2023 | vauthors = Turner NC, Oliveira M, Howell SJ, Dalenc F, Cortes J, Gomez Moreno HL, Hu X, Jhaveri K, Krivorotko P, Loibl S, Morales Murillo S, Okera M, Park YH, Sohn J, Toi M, Tokunaga E, Yousef S, Zhukova L, de Bruin EC, Grinsted L, Schiavon G, Foxley A, Rugo HS | journal = New England Journal of Medicine | volume = 388 | issue = 22 | pages = 2058–2070 | pmid = 37256976 | s2cid = 259002400 | pmc = 11335038 }} It is taken by mouth.
The most common adverse reactions include diarrhea, cutaneous adverse reactions, increased random glucose, decreased lymphocytes, decreased hemoglobin, increased fasting glucose, nausea, fatigue, decreased leukocytes, increased triglycerides, decreased neutrophils, increased creatinine, vomiting, and stomatitis.
In November 2023, capivasertib was approved in the United States for people with hormone receptor-positive, human epidermal growth factor receptor 2-negative breast cancer when used in combination with fulvestrant.{{cite web | title=FDA approves capivasertib with fulvestrant for breast cancer | website=U.S. Food and Drug Administration | date=16 November 2023 | url=https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-capivasertib-fulvestrant-breast-cancer | access-date=17 November 2023 | archive-date=17 November 2023 | archive-url=https://web.archive.org/web/20231117090823/https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-capivasertib-fulvestrant-breast-cancer | url-status=live }} {{PD-notice}}{{cite web | title=Oncology (Cancer) / Hematologic Malignancies Approval Notifications | website=U.S. Food and Drug Administration | date=16 November 2023 | url=https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications | access-date=17 November 2023 | archive-date=17 November 2023 | archive-url=https://web.archive.org/web/20231117055636/https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications | url-status=dead }}{{cite press release | title=Truqap (capivasertib) plus Faslodex approved in the US for patients with advanced HR-positive breast cancer | website=AstraZeneca | date=17 November 2023 | url=https://www.astrazeneca.com/media-centre/press-releases/2023/truqap-approved-in-us-for-hr-plus-breast-cancer.html | access-date=17 November 2023 | archive-date=17 November 2023 | archive-url=https://web.archive.org/web/20231117090858/https://www.astrazeneca.com/media-centre/press-releases/2023/truqap-approved-in-us-for-hr-plus-breast-cancer.html | url-status=live }} The US Food and Drug Administration (FDA) considers it to be a first-in-class medication.{{cite report | title=New Drug Therapy Approvals 2023 | website=U.S. Food and Drug Administration (FDA) | date=January 2024 | url=https://www.fda.gov/media/175253/download | format=PDF | access-date=9 January 2024 | archive-url=https://web.archive.org/web/20240110032419/https://www.fda.gov/media/175253/download | archive-date=10 January 2024 | url-status=live }} In April 2025 capivasertib, used alongside fulvestrant, was approved by the NHS in the UK.{{Cite web |last=England |first=N. H. S. |date=2025-04-11 |title=NHS England » Targeted breast cancer treatment approved for routine NHS use |url=https://www.england.nhs.uk/2025/04/targeted-breast-cancer-treatment-approved-for-routine-nhs-use/ |access-date=2025-04-17 |website=www.england.nhs.uk |language=en-US}}
Medical uses
Capivasertib, used in combination with fulvestrant (Faslodex), is indicated for adults with hormone receptor-positive, human epidermal growth factor receptor 2-negative locally advanced or metastatic breast cancer with one or more PIK3CA/AKT1/PTEN-alterations, as detected by an FDA-approved test, following progression on at least one endocrine-based regimen in the metastatic setting or recurrence on or within twelve months of completing adjuvant therapy.
History
Efficacy was evaluated in CAPItello-291 (NCT04305496), a randomized, double-blind, placebo-controlled, multicenter trial in 708 participants with locally advanced or metastatic HR-positive, HER2-negative breast cancer, of which 289 participants had tumors with PIK3CA/AKT1/PTEN-alterations. All participants were required to have progression on aromatase inhibitor-based treatment. Participants could have received up to two prior lines of endocrine therapy and up to one line of chemotherapy for locally advanced or metastatic disease.{{Cite report |url=https://clinicaltrials.gov/study/NCT04305496 |title=A Phase III Double-blind Randomised Study Assessing the Efficacy and Safety of Capivasertib + Fulvestrant Versus Placebo + Fulvestrant as Treatment for Locally Advanced (Inoperable) or Metastatic Hormone Receptor Positive, Human Epidermal Growth Factor Receptor 2 Negative (HR+/HER2-) Breast Cancer Following Recurrence or Progression On or After Treatment With an Aromatase Inhibitor |last=AstraZeneca |date=2023-05-26 |publisher=clinicaltrials.gov |issue=NCT04305496 |access-date=28 November 2024 |archive-date=2 August 2024 |archive-url=https://web.archive.org/web/20240802124432/https://clinicaltrials.gov/study/NCT04305496 |url-status=live }}
Society and culture
= Legal status =
Capivasertib was approved for medical use in the United States in November 2023. The FDA granted the application for capivasertib fast track designation.
In April 2024, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Truqap, intended for the treatment of locally advanced or metastatic breast cancer with one or more PIK3CA/AKT1/PTEN alterations.{{cite press release | title=Meeting highlights from the Committee for Medicinal Products for Human Use (CHMP) 22-25 April 2024 | website=European Medicines Agency | date=26 April 2024 | url=https://www.ema.europa.eu/en/news/meeting-highlights-committee-medicinal-products-human-use-chmp-22-25-april-2024 | access-date=13 June 2024 | archive-date=5 July 2024 | archive-url=https://web.archive.org/web/20240705192841/https://www.ema.europa.eu/en/news/meeting-highlights-committee-medicinal-products-human-use-chmp-22-25-april-2024 | url-status=live }} The applicant for this medicinal product is AstraZeneca AB.{{cite web | title=Truqap EPAR | website=European Medicines Agency | date=25 April 2024 | url=https://www.ema.europa.eu/en/medicines/human/EPAR/truqap | access-date=27 April 2024 | archive-date=30 April 2024 | archive-url=https://web.archive.org/web/20240430024450/https://www.ema.europa.eu/en/medicines/human/EPAR/truqap | url-status=live }} Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged. Capivasertib was approved for medical use in the European Union in June 2024.{{cite web | title=Truqap PI | website=Union Register of medicinal products | date=18 June 2024 | url=https://ec.europa.eu/health/documents/community-register/html/h1820.htm | access-date=5 July 2024}}
References
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External links
- {{ClinicalTrialsGov|NCT04305496|Capivasertib+Fulvestrant vs Placebo+Fulvestrant as Treatment for Locally Advanced (Inoperable) or Metastatic HR+/HER2- Breast Cancer (CAPItello-291)}}
{{Targeted cancer therapeutic agents}}
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Category:Protein kinase inhibitors