Gedatolisib
Highest phase reached
Phase 3
Drug type
Small molecule
- Listing at source
- Listed
- Highest phase reached
- Phase 3
- Drug type
- Small molecule
- Drug name
- Gedatolisib
- Molecular weight
- 615.74
- Structure (SMILES)
- CN(C)C1CCN(C(=O)c2ccc(NC(=O)Nc3ccc(-c4nc(N5CCOCC5)nc(N5CCOCC5)n4)cc3)cc2)CC1
- gedatolisib
- Gedatolisib
- gedatolisib [INN]
- GEDATOLISIB [USAN]
- Gedatolisib [WHO-DD]
- gedatolisib inn
- gedatolisib usan
- gedatolisib who dd
- pf 05212384
- PF-05212384
- PF-05212384 (also known as PKI-587)
- PF-05212384 (gedatolisib)
- pki 587
- PKI-587
- revtorpyk
- REVTORPYK
- CAS registry numbers
- 1197160-78-3
- ChEMBL ID
- CHEMBL592445
- InChIKey
- DWZAEMINVBZMHQ-UHFFFAOYSA-N
- PubChem compound IDs
- 44516953
- FDA ingredient codes (UNII)
- 96265TNH2R
- Patents
- 0
- Designations
- 1
- First in class
- No
- Fast track
- No
- Breakthrough designation
- Yes
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Pharmacology name
- gedatolisib
- Type
- Synthetic organic
- Drug name stem
- -lisib
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha
- Gene symbol
- PIK3CA
- Protein identifier
- P42336
- Median affinity
- 9.4
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- mechanistic target of rapamycin kinase
- Gene symbol
- MTOR
- Protein identifier
- P42345
- Median affinity
- 8.8
- Affinity units
- pIC50
- Primary target
- Yes
- Mechanism
- PI3-kinase class I inhibitor
- Action type
- Inhibitor
- Target
- PI3-kinase class I
- Protein identifier
- O00329
- Mechanism
- PI3-kinase class I inhibitor
- Action type
- Inhibitor
- Target
- PI3-kinase class I
- Protein identifier
- O00459
- Mechanism
- PI3-kinase class I inhibitor
- Action type
- Inhibitor
- Target
- PI3-kinase class I
- Protein identifier
- P27986
- Mechanism
- PI3-kinase class I inhibitor
- Action type
- Inhibitor
- Target
- PI3-kinase class I
- Protein identifier
- P42336
- Mechanism
- PI3-kinase class I inhibitor
- Action type
- Inhibitor
- Target
- PI3-kinase class I
- Protein identifier
- P42338
- Mechanism
- PI3-kinase class I inhibitor
- Action type
- Inhibitor
- Target
- PI3-kinase class I
- Protein identifier
- P48736
- Mechanism
- PI3-kinase class I inhibitor
- Action type
- Inhibitor
- Target
- PI3-kinase class I
- Protein identifier
- Q8WYR1
- Mechanism
- PI3-kinase class I inhibitor
- Action type
- Inhibitor
- Target
- PI3-kinase class I
- Protein identifier
- Q92569
- Mechanism
- Serine/threonine-protein kinase mTOR inhibitor
- Action type
- Inhibitor
- Target
- Serine/threonine-protein kinase mTOR
- Protein identifier
- P42345
- Mechanism
- PI3-kinase class I inhibitor
- Action type
- Inhibitor
- Target
- PI3-kinase class I
- Mechanism
- Serine/threonine-protein kinase mTOR inhibitor
- Action type
- Inhibitor
- Target
- Serine/threonine-protein kinase mTOR
- Condition
- Myelodysplastic Syndromes
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000198
- Subject identifier
- D009190
- Condition
- Leukemia, Myeloid, Acute
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000222
- Subject identifier
- D015470
- Condition
- Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Endometrial Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0004230
- Subject identifier
- D016889
- Condition
- Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0004992
- Subject identifier
- D009369
- Condition
- Breast Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0007254
- Subject identifier
- D001943
- Condition identifier
- EFO_0000198
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000222
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000616
- Highest recorded phase
- 1
- Condition identifier
- EFO_0003060
- Condition identifier
- EFO_0004230
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002447
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004992
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005070
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005097
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005170
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005192
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005206
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005233
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005494
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005575
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005627
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0007254
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0008170
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0008315
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0008433
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0009831
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0011962
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0018177
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0018874
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0018881
- Highest recorded phase
- 2
And 1 more, listed on the interactive page.
- Event
- escherichia bacteraemia
- Reports
- 5
- Reporting signal score
- 31.1533
- Event
- hyperglycaemia
- Reports
- 5
- Reporting signal score
- 17.1313
- NCT00940498
- NCT01920061
- NCT01347866
- NCT01420081
- NCT02438761
- NCT02626507
- NCT02684032
- NCT03243331
- NCT03400254
- NCT03698383
- NCT05501886
- NCT02920450
- Hydrogen bond acceptors
- 10
- Hydrogen bond donors
- 2
- Polar surface area
- 128.29
- Calculated partition coefficient (ALogP)
- 3.02
- Calculated partition coefficient (XLogP)
- 2.4
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 1
- Rotatable bonds
- 7
- Heavy atoms
- 45
- Molecular formula
- C32H41N9O4
- Monoisotopic mass
- 615.32815082
- Natural product
- Yes
- Recorded assays
- 941
- Active assays
- 375
- Confirmatory
- Other
- Screening
- Protein Kinase Inhibitors
Solubility
- Median
- 14.5
- Mean
- 14.5
- Minimum
- 14
- Maximum
- 15
- Unit
- ug/mL
- Assays
- 2
- Standard deviation
- 0.707107
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- Solubility
Related records
Trials (22)
- A Study Of PF-05212384 In Combination With Other Anti-Tumor Agents and in Combination With Cisplatin in Patients With Triple Negative Breast Cancer in an Expansion Arm (TNBC)
- A Study Of PF-05212384 Plus FOLFIRI Versus Bevacizumab Plus FOLFIRI In Metastatic Colorectal Cancer
- A Study Of PF-05212384 Plus Irinotecan Vs Cetuximab Plus Irinotecan In Patients With KRAS And NRAS Wild Type Metastatic Colorectal Cancer
- A Study Of Two Dual PI3K/mTOR Inhibitors, PF-04691502 And PF-05212384 In Patients With Recurrent Endometrial Cancer
- A Study To Assess The Tolerability And Clinical Activity Of Gedatolisib In Combination With Palbociclib/Letrozole Or Palbociclib/Fulvestrant In Women With Metastatic Breast Cancer
- An Initial Safety Study of Gedatolisib Plus PTK7-ADC for Metastatic Triple-negative Breast Cancer
- Clinical Study Of PI3K/mTOR Inhibitors In Combination With An Oral MEK Inhibitor Or Irinotecan In Patients With Advanced Cancer
- Dose Finding Study Of PF-05212384 With Paclitaxel And Carboplatin In Patients With Advanced Solid Tumor
- Expanded Access Protocol for Subjects Previously Treated With Gedatolisib in B2151009
- Gedatolisib in Combination With Darolutamide in Metastatic Castration-Resistant Prostate Cancer
- Gedatolisib Plus Fulvestrant With or Without Palbociclib vs Standard-of-Care for the Treatment of Patients With Advanced or Metastatic HR+/HER2- Breast Cancer (VIKTORIA-1)
- Gedatolisib Plus Talazoparib in Advanced Triple Negative or BRCA1/2 Positive, HER2 Negative Breast Cancers
- Gedatolisib, Hydroxychloroquine or the Combination for Prevention of Recurrent Breast Cancer ("GLACIER")
- Investigation Of The Metabolism, And Excretion Of [14c]-PF-05212384 In Healthy Male Volunteers
- PF-05212384 (PKI-587) for t-AML/MDS or de Novo Relapsed or Refractory Acute Myeloid Leukemia (AML) (LAM-PIK)
- Phase 3 Study of Gedatolisib as First-Line Treatment for Patients With HR-Positive, HER2-Negative Advanced Breast Cancer (VIKTORIA-2)
- Phase I Study of Combination of Gedatolisib With Palbociclib and Faslodex in Patients With ER+/HER2- Breast Cancer
- Phase II Study of Herzuma® Plus Gedatolisib in Patients With HER-2 Positive Metastatic Breast Cancer
- RESOLVE: Abemaciclib + Letrozole +/- Metformin or Gedatolisib in Endometrial Cancer
- Study of Paclitaxel, Carboplatin, and PF-05212384 in Advanced or Metastatic NSCLC (UF-STO-LUNG-002)
In development for (7)
- Acute myeloid leukemia Phase 2
- Breast cancer Phase 3
- Cancer Phase 1
- Endometrial carcinoma Phase 2
- Myelodysplastic syndrome Phase 2
- Neoplasm Phase 1
- Non-small cell lung carcinoma Phase 1
Targets (9)
- MTOR Serine/threonine-protein kinase mTOR inhibitor
- PIK3CA PI3-kinase class I inhibitor
- PIK3CB PI3-kinase class I inhibitor
- PIK3CD PI3-kinase class I inhibitor
- PIK3CG PI3-kinase class I inhibitor
- PIK3R1 PI3-kinase class I inhibitor
- PIK3R2 PI3-kinase class I inhibitor
- PIK3R3 PI3-kinase class I inhibitor
- PIK3R5 PI3-kinase class I inhibitor