Capivasertib
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Also known as AZC5363Azd 5363Azd-5363AZD5363TruqapCAPIVASERTIB (AZD5363)
Summary
Capivasertib (CHEMBL2325741) is an approved small-molecule antineoplastic agent (ATC L01EX27) targeting AKT1, AKT2, and AKT3; indicated across 19 conditions including neoplasm and breast neoplasm; with CIViC clinical evidence for 39 variant-indication associations (e.g. AKT1 E17K in her2-receptor negative breast cancer).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01EX27
- Targets: 3 (AKT1, AKT2, AKT3)
- Indications: 19 conditions
- Clinical trials: 55
- Precision-oncology evidence (CIViC): 39 variant–indication associations
- Chemistry: 428.9 Da · C21H25ClN6O2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL2325741 |
| Name | Capivasertib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 25227436 |
| ChEBI | CHEBI:229222 |
| ATC | L01EX27 |
| Molecular formula | C21H25ClN6O2 |
| Molecular weight | 428.9 |
| InChIKey | JDUBGYFRJFOXQC-KRWDZBQOSA-N |
SMILES: C1CN(CCC1(C(=O)N[C@@H](CCO)C2=CC=C(C=C2)Cl)N)C3=NC=NC4=C3C=CN4
IUPAC name: 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide
ChEBI definition: An aminopiperidine that is piperidine substituted by 7H-pyrrolo[2,3-d]pyrimidin-4-yl, amino, and [(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]aminocarbonyl groups at positions 1, 4, and 4, respectively. It is a pan-AKT kinase inhibitor used in combination with fulvestrant for the treatment of adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, locally advanced or metastatic breast cancer with one or more PIK3CA/AKT1/PTEN-alterations.
Pharmacological roles (ChEBI): antineoplastic agent, EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor.
Also known as: AZC5363, Azd 5363, Azd-5363, AZD-5363, AZD5363, Capivasertib, Truqap, CAPIVASERTIB, AZD 5363, TRUQAP, CAPIVASERTIB (AZD5363)
Patent coverage: 843 distinct patent families (2,157 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 1,916 (89%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| AKT1 | AKT serine/threonine kinase 1 | Inhibition | 7.59 | 3.4% | P31749 |
| AKT2 | AKT serine/threonine kinase 2 | Inhibition | 8.1 | 2.6% | P31751 |
| AKT3 | AKT serine/threonine kinase 3 | Inhibition | 8.1 | 0.2% | Q9Y243 |
Broader ChEMBL bioactivity targets: 29 (assay-derived). Sample: Proto-oncogene tyrosine-protein kinase receptor Ret, Serine/threonine-protein kinase AKT, 5’-AMP-activated protein kinase subunit gamma-1, RAC-beta serine/threonine-protein kinase, 5’-AMP-activated protein kinase subunit gamma-2, Serine/threonine-protein kinase D3, Mitogen-activated protein kinase kinase kinase 11, cAMP-dependent protein kinase catalytic subunit beta, Rho-associated protein kinase 2, Protein kinase C alpha type.
Bioactivity
ChEMBL activities: 55 potent at pChembl ≥ 5 of 56 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| AKT1 | 9.05 | IC50 | 0.9 | nM | CHEMBL_ACT_26316467 |
| AKT1 | 9 | IC50 | 1 | nM | CHEMBL_ACT_26214208 |
| AKT1 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_12662154 |
| AKT1 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_22784728 |
| AKT1 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_25872909 |
| AKT1 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_25903352 |
| AKT1 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_25905435 |
| AKT1 | 8.49 | IC50 | 3.2 | nM | CHEMBL_ACT_27965993 |
| AKT1 | 8.49 | IC50 | 3.2 | nM | CHEMBL_ACT_28603706 |
| AKT2 | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_26214223 |
| AKT2 | 8.15 | IC50 | 7 | nM | CHEMBL_ACT_22784729 |
| AKT3 | 8.15 | IC50 | 7 | nM | CHEMBL_ACT_22784730 |
| AKT2 | 8.15 | IC50 | 7 | nM | CHEMBL_ACT_25905436 |
| AKT3 | 8.15 | IC50 | 7 | nM | CHEMBL_ACT_25905437 |
| AKT3 | 8.1 | IC50 | 8 | nM | CHEMBL_ACT_12662098 |
| AKT2 | 8.1 | IC50 | 8 | nM | CHEMBL_ACT_12662126 |
| AKT1 | 8.1 | IC50 | 8 | nM | CHEMBL_ACT_23265862 |
| AKT2 | 8.1 | IC50 | 8 | nM | CHEMBL_ACT_25872912 |
| AKT3 | 8.1 | IC50 | 8 | nM | CHEMBL_ACT_25872915 |
| AKT1 | 8.1 | IC50 | 8 | nM | CHEMBL_ACT_25903353 |
| AKT2 | 8.1 | IC50 | 8 | nM | CHEMBL_ACT_25903354 |
| AKT3 | 8.1 | IC50 | 8 | nM | CHEMBL_ACT_26214238 |
| AKT1 | 7.89 | IC50 | 13 | nM | CHEMBL_ACT_29055322 |
| AKT1 | 7.59 | IC50 | 25.43 | nM | CHEMBL_ACT_19274123 |
| AKT1 | 7.47 | IC50 | 34 | nM | CHEMBL_ACT_16589678 |
| ROCK2 | 7.25 | IC50 | 56 | nM | CHEMBL_ACT_12662030 |
| AKT3 | 7.24 | IC50 | 57 | nM | CHEMBL_ACT_29055324 |
| AKT2 | 7.18 | IC50 | 66 | nM | CHEMBL_ACT_29055323 |
| PRKACB | 6.62 | Kd | 239 | nM | CHEMBL_ACT_17928705 |
| PRKG1 | 6.53 | Kd | 297 | nM | CHEMBL_ACT_17931902 |
Target pathways
Aggregated over 3 target gene(s): AKT1, AKT2, AKT3.
Top Reactome pathways
127 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Apoptosis | 3 | AKT1, AKT2, AKT3 |
| Intrinsic Pathway for Apoptosis | 3 | AKT1, AKT2, AKT3 |
| Activation of BAD and translocation to mitochondria | 3 | AKT1, AKT2, AKT3 |
| Activation of BH3-only proteins | 3 | AKT1, AKT2, AKT3 |
| Signaling by ERBB2 | 3 | AKT1, AKT2, AKT3 |
| PIP3 activates AKT signaling | 3 | AKT1, AKT2, AKT3 |
| Developmental Biology | 3 | AKT1, AKT2, AKT3 |
| Cytokine Signaling in Immune system | 3 | AKT1, AKT2, AKT3 |
| Adaptive Immune System | 3 | AKT1, AKT2, AKT3 |
| Downregulation of ERBB2:ERBB3 signaling | 3 | AKT1, AKT2, AKT3 |
| Signal Transduction | 3 | AKT1, AKT2, AKT3 |
| Cell Cycle | 3 | AKT1, AKT2, AKT3 |
| Disease | 3 | AKT1, AKT2, AKT3 |
| MTOR signalling | 3 | AKT1, AKT2, AKT3 |
| Inhibition of TSC complex formation by AKT (PKB) | 3 | AKT1, AKT2, AKT3 |
| Immune System | 3 | AKT1, AKT2, AKT3 |
| Regulation of beta-cell development | 3 | AKT1, AKT2, AKT3 |
| Signaling by VEGF | 3 | AKT1, AKT2, AKT3 |
| AKT phosphorylates targets in the cytosol | 3 | AKT1, AKT2, AKT3 |
| AKT phosphorylates targets in the nucleus | 3 | AKT1, AKT2, AKT3 |
| Negative regulation of the PI3K/AKT network | 3 | AKT1, AKT2, AKT3 |
| Membrane Trafficking | 3 | AKT1, AKT2, AKT3 |
| Regulation of gene expression in beta cells | 3 | AKT1, AKT2, AKT3 |
| AKT-mediated inactivation of FOXO1A | 3 | AKT1, AKT2, AKT3 |
| Generic Transcription Pathway | 3 | AKT1, AKT2, AKT3 |
| PI3K/AKT Signaling in Cancer | 3 | AKT1, AKT2, AKT3 |
| Cellular responses to stress | 3 | AKT1, AKT2, AKT3 |
| Transcriptional Regulation by TP53 | 3 | AKT1, AKT2, AKT3 |
| Signaling by GPCR | 3 | AKT1, AKT2, AKT3 |
| GPCR downstream signalling | 3 | AKT1, AKT2, AKT3 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| protein phosphorylation | 3 |
| signal transduction | 3 |
| insulin receptor signaling pathway | 3 |
| positive regulation of cell migration | 3 |
| intracellular signal transduction | 3 |
| negative regulation of apoptotic process | 3 |
| positive regulation of blood vessel endothelial cell migration | 3 |
| negative regulation of PERK-mediated unfolded protein response | 3 |
| positive regulation of endothelial cell proliferation | 2 |
| glycogen biosynthetic process | 2 |
| glucose metabolic process | 2 |
| regulation of translation | 2 |
| negative regulation of long-chain fatty acid import across plasma membrane | 2 |
| positive regulation of glucose metabolic process | 2 |
| regulation of cell migration | 2 |
Indications & clinical
Indications
19 indications (4 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| neoplasm | 4 | MONDO:0005070 | EFO:0000616 |
| breast neoplasm | 4 | MONDO:0021100 | EFO:0003869 |
| adenocarcinoma | 2 | MONDO:0004970 | EFO:0000228 |
| gastric adenocarcinoma | 2 | MONDO:0005036 | EFO:0000503 |
| prostate adenocarcinoma | 2 | MONDO:0005082 | EFO:0000673 |
| squamous cell carcinoma | 2 | MONDO:0005096 | EFO:0000707 |
| non-small cell lung carcinoma | 2 | MONDO:0005233 | EFO:0003060 |
| gastric neoplasm | 2 | MONDO:0021085 | MONDO:0001056 |
| plasma cell myeloma | 2 | MONDO:0009693 | EFO:0001378 |
| neoplasm of mature B-cells | 2 | MONDO:0004949 | EFO:0000096 |
| triple-negative breast carcinoma | 2 | MONDO:0005494 | EFO:0005537 |
| meningioma | 2 | MONDO:0016642 | MONDO:0850302 |
| hereditary breast ovarian cancer syndrome | 1 | MONDO:0003582 | Orphanet:145 |
| lymphoid neoplasm | 1 | MONDO:0005157 | EFO:0001642 |
| tumor of uterus | 1 | MONDO:0021353 | EFO:0003859 |
4 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 55.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 21 |
| PHASE1 | 17 |
| PHASE3 | 9 |
| PHASE1/PHASE2 | 8 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT03997123 | PHASE3 | ACTIVE_NOT_RECRUITING | Capivasertib+Paclitaxel as First Line Treatment for Patients With Locally Advanced or Metastatic TNBC |
| NCT04305496 | PHASE3 | ACTIVE_NOT_RECRUITING | Capivasertib+Fulvestrant vs Placebo+Fulvestrant as Treatment for Locally Advanced (Inoperable) or Metastatic HR+/HER2- Breast Cancer |
| NCT04493853 | PHASE3 | ACTIVE_NOT_RECRUITING | Capivasertib+Abiraterone as Treatment for Patients With Metastatic Hormone-sensitive Prostate Cancer and PTEN Deficiency |
| NCT04862663 | PHASE3 | RECRUITING | Capivasertib + CDK4/6i + Fulvestrant for Advanced/Metastatic HR+/HER2- Breast Cancer (CAPItello-292) |
| NCT05348577 | PHASE3 | ACTIVE_NOT_RECRUITING | Study of Capivasertib + Docetaxel vs Placebo + Docetaxel as Treatment for Metastatic Castration Resistant Prostate Cancer (mCRPC) |
| NCT06635447 | PHASE3 | ACTIVE_NOT_RECRUITING | Capivasertib+Fulvestrant asTreatment for Locally Advanced(Inoperable) or Metastatic HR+/HER2- Breast Cancer in Chinese Patients |
| NCT06764186 | PHASE3 | ACTIVE_NOT_RECRUITING | 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 |
| NCT06982521 | PHASE3 | RECRUITING | Phase 3 Study of RLY-2608 + Fulvestrant vs Capivasertib + Fulvestrant as Treatment for Locally Advanced or Metastatic PIK3CA-mutant HR+/HER2- Breast Cancer |
| NCT07281833 | PHASE3 | RECRUITING | Phase III Study to Evaluate the Safety, Efficacy, and Impact on Quality of Life of Capivasertib Alongside Standard-of-care Endocrine Treatment in Patients With HR+/HER2- Advanced Breast Cancer and Progression on Prior Endocrine-based Treatment |
| NCT01992952 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Fulvestrant +/- Akt Inhibition in Advanced Aromatase Inhibitor Resistant Breast Cancer |
| NCT02299999 | PHASE2 | ACTIVE_NOT_RECRUITING | SAFIR02_Breast - Efficacy of Genome Analysis as a Therapeutic Decision Tool for Patients With Metastatic Breast Cancer |
| NCT02465060 | PHASE2 | ACTIVE_NOT_RECRUITING | Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial) |
| NCT02523014 | PHASE2 | RECRUITING | Vismodegib, FAK Inhibitor GSK2256098, Capivasertib, and Abemaciclib in Treating Patients With Progressive Meningiomas |
| NCT02813135 | PHASE1/PHASE2 | RECRUITING | European Proof-of-Concept Therapeutic Stratification Trial of Molecular Anomalies in Relapsed or Refractory Tumors |
| NCT03660826 | PHASE2 | ACTIVE_NOT_RECRUITING | Testing the Combination of Olaparib and Durvalumab, Cediranib and Durvalumab, Olaparib and Capivasertib, and Cediranib Alone in Recurrent or Refractory Endometrial Cancer Following the Earlier Phase of the Study That Tested Olaparib and Cediranib in Comparison to Cediranib Alone, and Olaparib Alone |
| NCT03742102 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | A Study of Novel Anti-cancer Agents in Patients With Metastatic Triple Negative Breast Cancer |
| NCT04439123 | PHASE2 | ACTIVE_NOT_RECRUITING | Testing AZD5363 as a Potential Targeted Treatment in Cancers With AKT Genetic Changes (MATCH-Subprotocol Y) |
| NCT05563220 | PHASE1/PHASE2 | RECRUITING | Open-Label Umbrella Study To Evaluate Safety And Efficacy Of Elacestrant In Various Combination In Participants With Metastatic Breast Cancer |
| NCT05593497 | PHASE2 | RECRUITING | 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 |
| NCT05720260 | PHASE2 | RECRUITING | Immunotherapy, Hormone Therapy, and AKT Inhibitor for Premenopausal ER Positive MBC |
| NCT06607757 | PHASE2 | RECRUITING | Capivasertib Plus Fulvestrant vs. Fulvestrant in Primary High-risk Lobular Breast Cancer |
| NCT07175415 | PHASE1/PHASE2 | NOT_YET_RECRUITING | HEM-iSMART E: Capivasertib + Venetoclax + Dexamethasone in Pediatric Patients With Relapsed or Refractory Hematological Malignancies |
| NCT07287917 | PHASE1/PHASE2 | RECRUITING | Study of AMXT 1501 and DFMO in Combination With Standard Therapies in Advanced Solid Tumors |
| NCT07294677 | PHASE1/PHASE2 | RECRUITING | CApivasertib, Venetoclax And Low-intensity chemotheRapY for Adults With ALL/LBL |
| NCT07426822 | PHASE2 | NOT_YET_RECRUITING | Rash & Diarrhea Prophylaxis With Capivasertib |
| NCT02077569 | PHASE2 | COMPLETED | AKT Inhibitor in Oestrogen Positive Breast Cancer |
| NCT02117167 | PHASE2 | COMPLETED | SAFIR02_Lung - Efficacy of Targeted Drugs Guided by Genomic Profiles in Metastatic NSCLC Patients |
| NCT02121639 | PHASE1/PHASE2 | COMPLETED | Open Label Phase I/Randomised,Double Blind Phase II Study in mCRPC of AZD5363 In Combination With DP Chemotherapy |
| NCT02423603 | PHASE2 | COMPLETED | PAKT: AZD5363 in Combination With Paclitaxel in Triple-Negative Advanced or Metastatic Breast Cancer |
| NCT02449655 | PHASE2 | TERMINATED | Trial of AZD5363 Plus Paclitaxel /AZD2014 Plus Paclitaxel in Biomarker Negative (PIK3CA/MEK/RAS/TP53/MET) Gastric Adenocarcinoma Patients as Second-line Chemotherapy |
| NCT02451956 | PHASE2 | COMPLETED | Study of AZD5363 in Combination With Paclitaxel, in Advanced Gastric Adenocarcinoma Patients Harboring PIK3CA Mutation and/or PIK3CA Amplification as a Second-line Chemotherapy |
| NCT02525068 | PHASE2 | UNKNOWN | A Study of Enzalutamide in Combination With AZD5363 in Patients With mCRPC |
| NCT02576444 | PHASE2 | TERMINATED | OLAParib COmbinations |
| NCT02664935 | PHASE2 | COMPLETED | National Lung Matrix Trial: Multi-drug Phase II Trial in Non-Small Cell Lung Cancer |
| NCT03182634 | PHASE2 | UNKNOWN | The UK Plasma Based Molecular Profiling of Advanced Breast Cancer to Inform Therapeutic CHoices (plasmaMATCH) Trial |
| NCT03801369 | PHASE2 | TERMINATED | AMTEC IIT: Phase 2 Multiarm Study in TNBC |
| NCT05008055 | PHASE2 | COMPLETED | Study of Capivasertib in Relapsed or Refractory B-cell Non-Hodgkin Lymphoma |
| NCT06613516 | PHASE2 | WITHDRAWN | Effect of Capivasertib on ctDNA in ER Positive Breast Cancer |
| NCT02208375 | PHASE1 | ACTIVE_NOT_RECRUITING | mTORC1/2 Inhibitor AZD2014 or the Oral AKT Inhibitor AZD5363 for Recurrent Endometrial and Ovarian |
| NCT03772561 | PHASE1 | RECRUITING | Phase I Study of AZD5363 + Olaparib + Durvalumab in Patients With Advanced or Metastatic Solid Tumor Malignancies |
Clinical evidence (CIViC)
Variant × indication × effect (39 predictive associations from 41 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| AKT1 E17K | Her2-receptor Negative Breast Cancer | Sensitivity/Response | Capivasertib + Fulvestrant | CIViC A | EID12181 |
| PIK3CA C420R | Her2-receptor Negative Breast Cancer | Sensitivity/Response | Capivasertib + Fulvestrant | CIViC A | EID12183 |
| PIK3CA E542K | Her2-receptor Negative Breast Cancer | Sensitivity/Response | Fulvestrant + Capivasertib | CIViC A | EID12184 |
| PIK3CA E545A | Her2-receptor Negative Breast Cancer | Sensitivity/Response | Fulvestrant + Capivasertib | CIViC A | EID12185 |
| PIK3CA E545D | Her2-receptor Negative Breast Cancer | Sensitivity/Response | Capivasertib + Fulvestrant | CIViC A | EID12186 |
| PIK3CA E545G | Her2-receptor Negative Breast Cancer | Sensitivity/Response | Fulvestrant + Capivasertib | CIViC A | EID12189 |
| PIK3CA E545K | Her2-receptor Negative Breast Cancer | Sensitivity/Response | Fulvestrant + Capivasertib | CIViC A | EID12188 |
| PIK3CA E545Q | Her2-receptor Negative Breast Cancer | Sensitivity/Response | Fulvestrant + Capivasertib | CIViC A | EID12187 |
| PIK3CA G1049R | Her2-receptor Negative Breast Cancer | Sensitivity/Response | Capivasertib + Fulvestrant | CIViC A | EID12198 |
| PIK3CA H1047L | Her2-receptor Negative Breast Cancer | Sensitivity/Response | Capivasertib + Fulvestrant | CIViC A | EID12197 |
| PIK3CA H1047R | Her2-receptor Negative Breast Cancer | Sensitivity/Response | Fulvestrant + Capivasertib | CIViC A | EID12196 |
| PIK3CA H1047Y | Her2-receptor Negative Breast Cancer | Sensitivity/Response | Capivasertib + Fulvestrant | CIViC A | EID12195 |
| PIK3CA M1043I | Her2-receptor Negative Breast Cancer | Sensitivity/Response | Capivasertib + Fulvestrant | CIViC A | EID12194 |
| PIK3CA M1043V | Her2-receptor Negative Breast Cancer | Sensitivity/Response | Fulvestrant + Capivasertib | CIViC A | EID12193 |
| PIK3CA Mutation OR PTEN Mutation OR AKT1 Mutation | Breast Cancer | Sensitivity/Response | Capivasertib + Fulvestrant | CIViC A | EID12020 |
| PIK3CA N345K | Her2-receptor Negative Breast Cancer | Sensitivity/Response | Capivasertib + Fulvestrant | CIViC A | EID12182 |
| PIK3CA Q546E | Her2-receptor Negative Breast Cancer | Sensitivity/Response | Fulvestrant + Capivasertib | CIViC A | EID12190 |
| PIK3CA Q546K | Her2-receptor Negative Breast Cancer | Sensitivity/Response | Capivasertib + Fulvestrant | CIViC A | EID12191 |
| PIK3CA Q546P | Her2-receptor Negative Breast Cancer | Sensitivity/Response | Capivasertib + Fulvestrant | CIViC A | EID12192 |
| PIK3CA R88Q | Her2-receptor Negative Breast Cancer | Sensitivity/Response | Capivasertib + Fulvestrant | CIViC A | EID12034 |
| AKT1 E17K | Cancer | Sensitivity/Response | Capivasertib | CIViC B | EID3039 +1 |
| PIK3CA Mutation | Cancer | Sensitivity/Response | Capivasertib | CIViC B | EID3040 +1 |
| AKT1 D323G | Breast Cancer | Sensitivity/Response | Capivasertib | CIViC C | EID10765 |
| AKT1 E17K | Breast Cancer | Sensitivity/Response | Capivasertib | CIViC C | EID709 |
| AKT1 L52R | Endometrial Cancer | Sensitivity/Response | Capivasertib | CIViC C | EID10762 |
| AKT2 L78_Q79ins | Prostate Cancer | Sensitivity/Response | Capivasertib | CIViC C | EID10763 |
| IRS2 Amplification | Prostate Cancer | Resistance | Capivasertib | CIViC C | EID10764 |
| AKT1 F55Y | Cancer | Sensitivity/Response | ARQ092 + Capivasertib | CIViC D | EID10766 |
| AKT1 P68-C77dup | Cancer | Sensitivity/Response | Capivasertib | CIViC D | EID10767 |
| KDM5C Loss-of-function AND ( PIK3CA E545K OR PIK3CA H1047R OR PTEN Loss ) | Estrogen-receptor Positive Breast Cancer | Sensitivity/Response | Capivasertib | CIViC D | EID12936 |
+9 more predictive associations (showing top 30 by level).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
41 molecules share ≥1 primary target. Top 41 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | AKT1, AKT2, AKT3 |
| AFURESERTIB | ChEMBL | Phase 3 | AKT1, AKT2, AKT3 |
| IPATASERTIB | ChEMBL | Phase 3 | AKT1, AKT2, AKT3 |
| LESTAURTINIB | ChEMBL | Phase 3 | AKT1, AKT2, AKT3 |
| MIRANSERTIB | ChEMBL | Phase 2 | AKT1, AKT2, AKT3 |
| MK-2206 | ChEMBL | Phase 2 | AKT1, AKT2, AKT3 |
| UPROSERTIB | ChEMBL | Phase 2 | AKT1, AKT2, AKT3 |
| Afatinib | PubChem | Approved | AKT1, AKT2, AKT3 |
| belumosudil | PubChem | Approved | AKT1, AKT2, AKT3 |
| Binimetinib | PubChem | Approved | AKT1, AKT2, AKT3 |
| Crizotinib | PubChem | Approved | AKT1, AKT2, AKT3 |
| dacomitinib | PubChem | Approved | AKT1, AKT2, AKT3 |
| Fostamatinib | PubChem | Approved | AKT1, AKT2, AKT3 |
| Idelalisib | PubChem | Approved | AKT1, AKT2, AKT3 |
| Pazopanib | PubChem | Approved | AKT1, AKT2, AKT3 |
| regorafenib | PubChem | Approved | AKT1, AKT2, AKT3 |
| Selumetinib | PubChem | Approved | AKT1, AKT2, AKT3 |
| Trametinib | PubChem | Approved | AKT1, AKT2, AKT3 |
| FASUDIL | ChEMBL | Phase 3 | AKT1, AKT3 |
| RUBOXISTAURIN | ChEMBL | Phase 3 | AKT2, AKT3 |
| LAUROGUADINE | ChEMBL | Phase 2 | AKT1, AKT2 |
| SOTRASTAURIN | ChEMBL | Phase 2 | AKT1, AKT2 |
| Gefitinib | PubChem | Approved | AKT2, AKT3 |
| MILTEFOSINE | ChEMBL | Phase 4 (approved) | AKT1 |
| NICLOSAMIDE | ChEMBL | Phase 4 (approved) | AKT1 |
| SUNITINIB | ChEMBL | Phase 4 (approved) | AKT2 |
| ENZASTAURIN | ChEMBL | Phase 3 | AKT3 |
| LINIFANIB | ChEMBL | Phase 3 | AKT1 |
| PERIFOSINE | ChEMBL | Phase 3 | AKT1 |
| QUERCETIN | ChEMBL | Phase 3 | AKT1 |
| EDELFOSINE | ChEMBL | Phase 2 | AKT1 |
| ELLAGIC ACID | ChEMBL | Phase 2 | AKT1 |
| KALAFUNGIN | ChEMBL | Phase 2 | AKT1 |
| PF-04691502 | ChEMBL | Phase 2 | AKT1 |
| PICTILISIB | ChEMBL | Phase 2 | AKT1 |
| RUPITASERTIB | ChEMBL | Phase 2 | AKT1 |
| SULFAETHIDOLE | ChEMBL | Phase 2 | AKT1 |
| Belzutifan | PubChem | Approved | AKT2 |
| Cobimetinib | PubChem | Approved | AKT3 |
| Fedratinib | PubChem | Approved | AKT3 |
| podofilox | PubChem | Approved | AKT1 |
Related Atlas pages
- Genes: AKT1, AKT2, AKT3
- Diseases: neoplasm, breast neoplasm, Her2-receptor negative breast cancer, breast carcinoma, cancer, endometrial carcinoma, prostate carcinoma, estrogen-receptor positive breast cancer
- Drugs: Midostaurin, Afuresertib, Ipatasertib, Lestaurtinib, Afatinib, belumosudil, Binimetinib, Crizotinib, dacomitinib, Fostamatinib, Idelalisib, Pazopanib, regorafenib, Selumetinib, Trametinib, Fasudil, Ruboxistaurin, Gefitinib, Miltefosine, Niclosamide, Sunitinib, Enzastaurin, Linifanib, Perifosine, Quercetin, Belzutifan, Cobimetinib, Fedratinib, podofilox
- Biomarker genes: PIK3CA