Capivasertib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2023
- First approval year
- 2023
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Capivasertib
- Molecular weight
- 428.92
- Structure (SMILES)
- NC1(C(=O)N[C@@H](CCO)c2ccc(Cl)cc2)CCN(c2nc[nH]c3nccc2-3)CC1
- truqap
- Truqap
- [14C]AZD5363 (Capivasertib)
- 14c azd5363 capivasertib
- azc5363
- AZC5363
- azd 5363
- Azd 5363
- AZD 5363
- Azd-5363
- AZD-5363
- azd5363
- AZD5363
- capivasertib
- Capivasertib
- CAPIVASERTIB
- CAPIVASERTIB (AZD5363)
- capivasertib [INN]
- CAPIVASERTIB [JAN]
- Capivasertib [MI]
- CAPIVASERTIB [USAN]
- Capivasertib [WHO-DD]
- capivasertib azd5363
- capivasertib inn
- capivasertib jan
- capivasertib mi
- capivasertib usan
And 3 more, listed on the interactive page.
- ATC classification codes
- L01EX27
Sources for recorded values
- CAS registry numbers
- 1143532-39-1
- ChEMBL ID
- CHEMBL2325741
- InChIKey
- JDUBGYFRJFOXQC-KRWDZBQOSA-N
- PubChem compound IDs
- 25227436
- RxNorm IDs (RxCUI)
- 2669967
- FDA ingredient codes (UNII)
- WFR23M21IE
- Applicant
- ASTRAZENECA
- Approval date
- 16 Nov 2023
- Application number
- NDA218197
- Status
- Authorised
- Status date
- 17 Jun 2024
- Authorisation date
- 17 Jun 2024
- Approved indications
- Truqap is indicated in combination with fulvestrant for the treatment of adult patients with oestrogen receptor (ER)-positive, HER2-negative locally advanced or metastatic breast cancer with one or more PIK3CA/AKT1/PTEN-alterations following recurrence or progression on or after an endocrine-based regimen. In pre- or perimenopausal women, Truqap plus fulvestrant should be combined with a luteinising hormone releasing hormone (LHRH) agonist. For men, administration of LHRH agonist according to current clinical practice standards should be considered.
- Product number
- EMEA/H/C/006017
- Authorisation holder
- AstraZeneca AB
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- Yes
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Breast Neoplasms
European medicines record
- Patents
- 7
- Designations
- 2
- Earliest recorded loss of exclusivity
- 16 Apr 2033
- First in class
- Yes
- Fast track
- Yes
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Pharmacology name
- capivasertib
- Type
- Synthetic organic
- Drug name stem
- -sertib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- AKT serine/threonine kinase 1
- Gene symbol
- AKT1
- Protein identifier
- P31749
- Median affinity
- 8.52
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- AKT serine/threonine kinase 2
- Gene symbol
- AKT2
- Protein identifier
- P31751
- Median affinity
- 8.1
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- AKT serine/threonine kinase 3
- Gene symbol
- AKT3
- Protein identifier
- Q9Y243
- Median affinity
- 8.1
- Affinity units
- pIC50
- Primary target
- Yes
- Mechanism
- Serine/threonine-protein kinase AKT inhibitor
- Action type
- Inhibitor
- Target
- Serine/threonine-protein kinase AKT
- Protein identifier
- P31749
- Mechanism
- Serine/threonine-protein kinase AKT inhibitor
- Action type
- Inhibitor
- Target
- Serine/threonine-protein kinase AKT
- Protein identifier
- P31751
- Mechanism
- Serine/threonine-protein kinase AKT inhibitor
- Action type
- Inhibitor
- Target
- Serine/threonine-protein kinase AKT
- Protein identifier
- Q9Y243
Open Targets mechanisms
- Mechanism
- Serine/threonine-protein kinase AKT inhibitor
- Action type
- Inhibitor
- Target
- Serine/threonine-protein kinase AKT
- Condition
- Lymphoma, Follicular
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000096
- Subject identifier
- D008224
- Condition
- Adenocarcinoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000228
- Subject identifier
- D000230
- Condition
- Stomach Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000503
- Subject identifier
- D013274
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000673
- Subject identifier
- D011471
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000707
- Subject identifier
- D002294
- Condition
- Multiple Myeloma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001378
- Subject identifier
- D009101
- Condition
- Hematologic Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001642
- Subject identifier
- D019337
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Uterine Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003859
- Subject identifier
- D014594
- Condition
- Breast Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0003869
- Subject identifier
- D001943
- Condition
- Triple Negative Breast Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005537
- Subject identifier
- D064726
- Condition
- Stomach Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0001056
- Subject identifier
- D013274
- Condition
- Uterine Cervical Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0002974
- Subject identifier
- D002583
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0004992
- Subject identifier
- D009369
- Condition
- Breast Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0007254
- Subject identifier
- D001943
- Condition
- Prostatic Neoplasms, Castration-Resistant
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0008315
- Subject identifier
- D064129
- Condition
- Meningioma
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0850302
- Subject identifier
- D008579
- Condition
- Hereditary Breast and Ovarian Cancer Syndrome
- Highest recorded phase
- 1
- Condition identifier
- Orphanet:145
- Subject identifier
- D061325
- Condition identifier
- EFO_0000096
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000673
- Highest recorded phase
- 2
- Condition identifier
- EFO_0001642
- Highest recorded phase
- 1
- Condition identifier
- EFO_0003869
- Condition identifier
- EFO_0005537
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0000873
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0001416
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0002974
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0004967
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0004992
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005036
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005062
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005070
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005233
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005494
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0007254
- Condition identifier
- MONDO_0007254
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0008170
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0008315
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0009693
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0011962
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0016642
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0017604
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0018876
- Highest recorded phase
- 2
And 4 more, listed on the interactive page.
Reported adverse events
- Event
- hyperglycaemia
- Reports
- 3
- Reporting signal score
- 9.01811
- NCT01226316
- NCT01353781
- NCT01895946
- NCT02338622
- NCT02576444
- NCT03772561
- NCT04742036
- NCT04958226
- NCT01625286
- NCT01992952
- NCT02077569
- NCT02299999
- NCT03182634
- NCT04305496
- NCT04862663
- NCT01692262
- NCT02121639
- NCT04087174
- NCT04493853
- NCT05348577
- NCT05593497
- NCT02117167
- NCT02664935
- NCT02208375
- NCT03801369
And 9 more, listed on the interactive page.
- Dose
- 400 mg
- Route
- Oral
- How often
- Twice daily for 4 days followed by 3 days off
Conditions of use
- Take with or without food
- Hydrogen bond acceptors
- 6
- Hydrogen bond donors
- 4
- Polar surface area
- 120.16
- Calculated partition coefficient (ALogP)
- 2.1
- Calculated partition coefficient (XLogP)
- 1.7
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 6
- Heavy atoms
- 30
- Molecular formula
- C21H25ClN6O2
- Monoisotopic mass
- 428.1727518
- Natural product
- Yes
- 0310-9500
- 0310-9501
- Recorded assays
- 1,025
- Active assays
- 241
- Confirmatory
- Other
- Screening
- Antineoplastic Agents
- Protein Kinase Inhibitors
These details could not be displayed.
Related records
Trials (62)
- A Multi-centre Study to Assess the Safety, Tolerability, and Pharmacokinetics of Capivasertib (AZD5363) in Combination With Novel Agents in Patients With Metastatic Prostate Cancer
- A Phase 1b Study of T-DXd Combinations in HER2-low Advanced or Metastatic Breast Cancer
- A Phase I Study to Investigate the Pharmacokinetics and Safety of Capivasertib in Participants With Moderate Hepatic Impairment
- A Phase IIIB Study to Evaluate the Use of Capivasertib in Combination With Fulvestrant in Patients With Advanced Breast Cancer Who Have Relapsed/Progressed on ET and CDK4/6 Inhibitor Reflecting Real World Clinical Practice in Spain
- A Single-Arm Phase II Study of Neoadjuvant Intensified Androgen Deprivation (Leuprolide and Abiraterone Acetate) in Combination With AKT Inhibition (Capivasertib) for High-Risk Localized Prostate Cancer With PTEN Loss
- A Study of Enzalutamide in Combination With AZD5363 in Patients With mCRPC
- A Study of Novel Anti-cancer Agents in Patients With Metastatic Triple Negative Breast Cancer
- A Study to Assess How Itraconazole Affects the Uptake and Elimination of Capivasertib in the Body
- A Study to Assess the Effect of Capivasertib on Midazolam in Patients With Advanced Solid Tumours
- A Study to Investigate the Absolute Bioavailability, Absorption, Metabolism, Distribution and Excretion of [14C]AZD5363 (Capivasertib)
- A Study to Investigate the Effect of Capivasertib on the Pharmacokinetics of Oral Dextromethorphan (CYP2D6 Substrate) in Healthy Participants
- A Study to Investigate the Effect of Capivasertib on the Pharmacokinetics of Oral Rosuvastatin in Healthy Participants
- AKT Inhibitor in Oestrogen Positive Breast Cancer
- AMTEC IIT: Phase 2 Multiarm Study in TNBC
- AZD5363 in Patients With Advanced Solid Tumors Harboring AKT Mutations
- Capivasertib + CDK4/6i + Fulvestrant for Advanced/Metastatic HR+/HER2- Breast Cancer (CAPItello-292)
- Capivasertib China PK Study
- Capivasertib Plus Fulvestrant vs. Fulvestrant in Primary High-risk Lobular Breast Cancer
- CApivasertib, Venetoclax And Low-intensity chemotheRapY for Adults With ALL/LBL
- Capivasertib+Abiraterone as Treatment for Patients With Metastatic Hormone-sensitive Prostate Cancer and PTEN Deficiency
Approved for (4)
In development for (15)
- Adenocarcinoma Phase 2
- Cervical cancer Phase 1
- Gastric adenocarcinoma Phase 2
- Gastric cancer Phase 2
- Hereditary breast ovarian cancer syndrome Phase 1
- Intracranial meningioma Phase 2
- Lymphoid neoplasm Phase 1
- Neoplasm of mature B-cells Phase 2
- Non-small cell lung carcinoma Phase 2
- Plasma cell myeloma Phase 2
- Prostate adenocarcinoma Phase 2
- Prostate cancer Phase 3
- Squamous cell carcinoma Phase 2
- Triple-negative breast carcinoma Phase 2
- Tumor of uterus Phase 1