Capivasertib

Capivasertib, sold under the brand name Truqap, is an anti-cancer medication used for the treatment of breast cancer.^[4][7] It is taken by mouth.^[4]

Capivasertib

Clinical data
Trade names	Truqap
Other names	AZD-5363, AZD5363
AHFS/Drugs.com
MedlinePlus	a623056
License data	US DailyMed: Capivasertib
Pregnancy category	AU: D[1]
Routes of administration	By mouth
Drug class	Threonine kinase inhibitor
ATC code	L01EX27 (WHO)
Legal status
Legal status	AU: S4 (Prescription only)[1][2] CA: ℞-only[3] US: ℞-only[4] EU: Rx-only[5][6]
Identifiers
IUPAC name 4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide
CAS Number	1143532-39-1
PubChem CID	25227436
DrugBank	DB12218
ChemSpider	28189073
UNII	WFR23M21IE
KEGG	D11371
ChEBI	CHEBI:229222
ChEMBL	ChEMBL2325741
PDB ligand	0XZ (PDBe, RCSB PDB)
CompTox Dashboard (EPA)	DTXSID40150710
ECHA InfoCard	100.208.066
Chemical and physical data
Formula	C21H25ClN6O2
Molar mass	428.92 g·mol−1
3D model (JSmol)	Interactive image
SMILES NC1(CCN(CC1)C1=C2C=CNC2=NC=N1)C(=O)N[C@@H](CCO)C1=CC=C(Cl)C=C1
InChI InChI=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 Key:JDUBGYFRJFOXQC-KRWDZBQOSA-N

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.^[8]

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.^[8][9][10] The US Food and Drug Administration (FDA) considers it to be a first-in-class medication.^[11] In April 2025 capivasertib, used alongside fulvestrant, was approved by the NHS in the UK.^[12]

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.^[4][8]

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.^[8] All participants were required to have progression on aromatase inhibitor-based treatment.^[8] 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.^[8][13]

Society and culture

Legal status

Capivasertib was approved for medical use in the United States in November 2023.^[8] The FDA granted the application for capivasertib fast track designation.^[11]

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.^[5][14] The applicant for this medicinal product is AstraZeneca AB.^[5] Capivasertib was approved for medical use in the European Union in June 2024.^[5][6]