Palbociclib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2015
- First approval year
- 2015
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Palbociclib
- Molecular weight
- 447.54
- Structure (SMILES)
- CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O
- ibrance
- Ibrance
- 100mg palbociclib
- 6 acetyl 8 cyclopentyl 5 methyl 2 5 1 piperazinyl 2 pyridinyl amino pyrido 2 3 d pyrimidin 7 8h one
- 6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one
- azd9833 with palbociclib
- ibrance
- Ibrance
- IBRANCE
- palbociclib
- Palbociclib
- PALBOCICLIB
- Palbociclib [INN]
- Palbociclib [JAN]
- Palbociclib [MI]
- Palbociclib [ORANGE BOOK]
- Palbociclib [USAN]
- Palbociclib [WHO-DD]
- Palbociclib 100mg
- Palbociclib 125mg
- Palbociclib 200mg
- Palbociclib 75 mg Capsule
- Palbociclib 75mg
- Palbociclib 75mg-125mg
- Palbociclib capsules
- palbociclib inn
- palbociclib isethionate
And 27 more, listed on the interactive page.
- ATC classification codes
- L01EF01
Sources for recorded values
- CAS registry numbers
- 571190-30-2
- ChEMBL ID
- CHEMBL189963
- InChIKey
- AHJRHEGDXFFMBM-UHFFFAOYSA-N
- PubChem compound IDs
- 5330286
- RxNorm IDs (RxCUI)
- 1601374
- FDA ingredient codes (UNII)
- G9ZF61LE7G
- Applicant
- PFIZER
- Approval date
- 3 Feb 2015
- Application number
- NDA207103
- Status
- Authorised
- Status date
- 9 Nov 2016
- Authorisation date
- 9 Nov 2016
- Approved indications
- Ibrance is indicated for the treatment of hormone receptor (HR) positive, human epidermal growth factor receptor 2 (HER2) negative locally advanced or metastatic breast cancer: in combination with an aromatase inhibitor; in combination with fulvestrant in women who have received prior endocrine therapy. In pre- or perimenopausal women, the endocrine therapy should be combined with a luteinizing hormone releasing hormone (LHRH) agonist.
- Product number
- EMEA/H/C/003853
- Authorisation holder
- Pfizer Europe MA EEIG
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 1
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Breast Neoplasms
European medicines record
- Patents
- 10
- Designations
- 5
- Earliest recorded loss of exclusivity
- 19 Feb 2037
- First in class
- Yes
- Fast track
- No
- Breakthrough designation
- Yes
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- Yes
- Availability
- Prescription only
- Pharmacology name
- palbociclib
- Type
- Synthetic organic
- Drug name stem
- -ciclib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- cyclin dependent kinase 4
- Gene symbol
- CDK4
- Protein identifier
- P11802
- Median affinity
- 7.36
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- cyclin dependent kinase 6
- Gene symbol
- CDK6
- Protein identifier
- Q00534
- Median affinity
- 7.44
- Affinity units
- pIC50
- Mechanism
- CDK6/cyclin D1 inhibitor
- Action type
- Inhibitor
- Target
- CDK6/cyclin D1
- Protein identifier
- P24385
- Mechanism
- CDK6/cyclin D1 inhibitor
- Action type
- Inhibitor
- Target
- CDK6/cyclin D1
- Protein identifier
- Q00534
- Mechanism
- Cyclin-dependent kinase 4/cyclin D1 inhibitor
- Action type
- Inhibitor
- Target
- Cyclin-dependent kinase 4/cyclin D1
- Protein identifier
- P11802
- Mechanism
- Cyclin-dependent kinase 4/cyclin D1 inhibitor
- Action type
- Inhibitor
- Target
- Cyclin-dependent kinase 4/cyclin D1
- Protein identifier
- P24385
- Mechanism
- CDK6/cyclin D1 inhibitor
- Action type
- Inhibitor
- Target
- CDK6/cyclin D1
- Mechanism
- Cyclin-dependent kinase 4/cyclin D1 inhibitor
- Action type
- Inhibitor
- Target
- Cyclin-dependent kinase 4/cyclin D1
- Action type
- Inhibitor
- Gene symbol
- CDK4
- Protein identifier
- P11802
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- CDK6
- Protein identifier
- Q00534
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- DYRK1A
- Protein identifier
- Q13627
- Organism
- Homo sapiens
- Target development level
- Chemical evidence
- Action type
- Inhibitor
- Gene symbol
- RPS6KA1
- Protein identifier
- Q15418
- Organism
- Homo sapiens
- Target development level
- Chemical evidence
- Condition
- Sarcoma, Ewing
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000174
- Subject identifier
- D012512
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000181
- Subject identifier
- D002294
- Condition
- Carcinoma, Hepatocellular
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000182
- Subject identifier
- D006528
- Condition
- Precursor Cell Lymphoblastic Leukemia-Lymphoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000220
- Subject identifier
- D054198
- Condition
- Leukemia, Myeloid, Acute
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000222
- Subject identifier
- D015470
- Condition
- Adenocarcinoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000228
- Subject identifier
- D000230
- Condition
- Breast Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000305
- Subject identifier
- D001943
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000349
- Subject identifier
- D002292
- Condition
- Carcinoma, Intraductal, Noninfiltrating
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000432
- Subject identifier
- D002285
- Condition
- Glioblastoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000519
- Subject identifier
- D005909
- Condition
- Liposarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000569
- Subject identifier
- D008080
- Condition
- Lymphoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000574
- Subject identifier
- D008223
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Oligodendroglioma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000630
- Subject identifier
- D009837
- Condition
- Oligodendroglioma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000632
- Subject identifier
- D009837
- Condition
- Osteosarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000637
- Subject identifier
- D012516
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000681
- Subject identifier
- D002292
- Condition
- Sarcoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000691
- Subject identifier
- D012509
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000707
- Subject identifier
- D002294
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000708
- Subject identifier
- D002294
- Condition
- Melanoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000756
- Subject identifier
- D008545
- Condition
- Ovarian Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001075
- Subject identifier
- D010051
- Condition
- Multiple Myeloma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001378
- Subject identifier
- D009101
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0002618
- Subject identifier
- D010190
- Condition
- Thymus Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002626
- Subject identifier
- D013953
And 28 more, listed on the interactive page.
- Condition identifier
- EFO_0000174
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000181
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000182
- Condition identifier
- EFO_0000220
- Condition identifier
- EFO_0000222
- Condition identifier
- EFO_0000305
- Condition identifier
- EFO_0000432
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000574
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000630
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000632
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000681
- Condition identifier
- EFO_0000691
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000708
- Condition identifier
- EFO_0000756
- Highest recorded phase
- 2
- Condition identifier
- EFO_0001378
- Highest recorded phase
- 2
- Condition identifier
- EFO_0002618
- Highest recorded phase
- 1
- Condition identifier
- EFO_0002626
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003085
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003086
- Highest recorded phase
- 1
- Condition identifier
- EFO_0003869
- Condition identifier
- EFO_0005922
- Highest recorded phase
- 2
- Condition identifier
- EFO_0005952
- Highest recorded phase
- 1
- Condition identifier
- EFO_0006318
- Highest recorded phase
- 1
And 101 more, listed on the interactive page.
- Event
- alopecia
- Reports
- 1,925
- Reporting signal score
- 2,918.85
- Event
- blood count abnormal
- Reports
- 599
- Reporting signal score
- 1,225.55
- Event
- bone marrow failure
- Reports
- 541
- Reporting signal score
- 768.66
- Event
- breast cancer metastatic
- Reports
- 315
- Reporting signal score
- 753.145
- Event
- constipation
- Reports
- 902
- Reporting signal score
- 444.547
- Event
- decreased appetite
- Reports
- 1,065
- Reporting signal score
- 674.937
- Event
- diarrhoea
- Reports
- 1,923
- Reporting signal score
- 435.04
- Event
- disease progression
- Reports
- 1,152
- Reporting signal score
- 1,237.73
- Event
- dry skin
- Reports
- 375
- Reporting signal score
- 320.641
- Event
- fatigue
- Reports
- 4,560
- Reporting signal score
- 3,684.64
- Event
- full blood count decreased
- Reports
- 550
- Reporting signal score
- 913.627
- Event
- hot flush
- Reports
- 561
- Reporting signal score
- 648.398
- Event
- leukopenia
- Reports
- 547
- Reporting signal score
- 414.329
- Event
- malignant neoplasm progression
- Reports
- 541
- Reporting signal score
- 409.825
- Event
- metastases to bone
- Reports
- 270
- Reporting signal score
- 406.267
- Event
- nausea
- Reports
- 2,582
- Reporting signal score
- 733.332
- Event
- neoplasm progression
- Reports
- 2,931
- Reporting signal score
- 9,391.03
- Event
- neutropenia
- Reports
- 2,834
- Reporting signal score
- 4,023.63
- Event
- neutrophil count decreased
- Reports
- 694
- Reporting signal score
- 879.545
- Event
- oral pain
- Reports
- 281
- Reporting signal score
- 357.677
- Event
- platelet count decreased
- Reports
- 694
- Reporting signal score
- 376.529
- Event
- red blood cell count decreased
- Reports
- 469
- Reporting signal score
- 674.32
- Event
- stomatitis
- Reports
- 997
- Reporting signal score
- 1,458.64
- Event
- tumour marker increased
- Reports
- 234
- Reporting signal score
- 607.197
- Event
- white blood cell count decreased
- Reports
- 3,283
- Reporting signal score
- 6,267.56
- NCT00141297
- NCT00420056
- NCT02159755
- NCT03478514
- NCT01209598
- NCT01356628
- NCT01522989
- NCT02925234
- NCT03065387
- NCT03239015
- NCT04185883
- NCT04423185
- NCT05178888
- NCT05867251
- NCT01684215
- NCT01740427
- NCT02297438
- NCT02530424
- NCT02690480
- NCT03220178
- NCT03284723
- NCT03304080
- NCT03423199
- NCT03447132
- NCT03900884
And 178 more, listed on the interactive page.
- Dose
- 125 mg
- Route
- Oral
- How often
- Once daily, 21 days on followed by 7 days off
Conditions of use
- Take with food
- Hydrogen bond acceptors
- 9
- Hydrogen bond donors
- 2
- Polar surface area
- 105.04
- Calculated partition coefficient (ALogP)
- 2.97
- Calculated partition coefficient (XLogP)
- 1.8
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 5
- Heavy atoms
- 33
- Molecular formula
- C24H29N7O2
- Monoisotopic mass
- 447.23827319
- Natural product
- Yes
- 0069-0187
- 0069-0188
- 0069-0189
- 0069-0284
- 0069-0486
- 0069-0688
- 63539-284
- 63539-486
- 63539-688
- Recorded assays
- 4,498
- Active assays
- 831
- Confirmatory
- Other
- Screening
- Antineoplastic Agents
- Protein Kinase Inhibitors
Oral bioavailability
- Median
- 46
- Mean
- 46
- Minimum
- 46
- Maximum
- 46
- Unit
- %
- Assays
- 2
- Standard deviation
- 0
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- F
Related records
Trials (362)
- "Neo-Adjuvant Treatment With Palbociclib: Effect on Ki67 and Apoptosis Before, During and After Treatment "
- A Biomarker Study of Palbociclib + Fulvestrant for Second, and Third Line of Postmenopausal Women With hr+/her2- Advanced Breast Cancer
- A Clinical Research Study to Determine Whether PD 0332991 May Be Effective in Treating Patients With Liver Cancer
- A Comparative Study of AZD9833 Plus Palbociclib Versus Anastrozole Plus Palbociclib in Patients With ER-Positive HER2 Negative Breast Cancer Who Have Not Received Any Systemic Treatment for Advanced Disease
- A Drug-Drug Interaction Study To Investigate The Potential For Multiple Doses Of Palbociclib (PD-0332991) To Alter The Pharmacokinetics Of Oral Midazolam In Adult Healthy Women of Non-Childbearing Potential.
- A First-in-human Dose Escalation and Expansion Study to Evaluate the Safety, and Tolerability of AZD8421 Alone or in Combination in Participants With Selected Advanced or Metastatic Solid Tumors
- A First-in-Human Study of D-0502 Alone and in Combination With Palbociclib in Women With Advanced or Metastatic ER-Positive and HER2-Negative Breast Cancer
- A Open Label Study of the Efficacy and Safety of PD0332991 a Selective Inhibitor of the Cyclin Dependent Kinases 4 and 6 in Patients With Recurrent Ovarian Cancer Demonstrating Rb-proficiency and Low p16 Expression
- A Phase 1 Study of BMS-986500 as Monotherapy or Combination Therapy in Advanced Solid Tumors
- A Phase 1 Study of Oral OP-1250 in Combination With Palbociclib in HR+/HER2- Breast Cancer Patients
- A Phase 1 Trial of TST of PD 0332991 Followed by Cytarabine and Mitoxantrone for Adults With Relapsed and Refractory Acute Leukemias and High-Risk Myelodysplasia
- A Phase 1/2 Trial of ARV-471 Alone and in Combination With Palbociclib (IBRANCE®) in Patients With ER+/HER2- Locally Advanced or Metastatic Breast Cancer
- A Phase I Clinical Study on SHR6390 in Healthy Chinese Volunteers
- A Phase Ib/II Study to Evaluate Multiple Combination Therapies of FWD1802 in Patients With ER+/HER2- BC
- A Phase II Randomized Study Evaluating the Biological and Clinical Effects of the Combination of Palbociclib With Letrozole as Neoadjuvant Therapy in Post-Menopausal Women With Estrogen-Receptor Positive Primary Breast Cancer
- A Phase II Study of Androgen Deprivation Therapy With or Without Palbociclib in RB-Positive Metastatic Prostate Cancer
- A Phase II Study of Palbociclib for Recurrent or Refractory Advanced Thymic Epithelial Tumor
- A Pilot Study To Investigate The Effect Of Concurrent Antacid Administration On The Bioavailability Of Six Experimental Formulations Of Palbociclib
- A Randomized Study Comparing the Immune Modulation Effect of Ribociclib, Palbociclib, and Abemaciclib in ER+/HER2- EBC
- A Randomized, Open-label, Multi-center Phase IV Study Evaluating Palbociclib Plus Endocrine Treatment Versus a Chemotherapy-based Treatment Strategy in Patients With Hormone Receptor Positive / HER2 Negative Breast Cancer in a Real World Setting (GBG 93 - PADMA Study).
Approved for (6)
- Breast cancer
- Breast carcinoma
- Breast neoplasm
- Cancer
- HER2 positive breast carcinoma
- Neoplasm
In development for (47)
- Acute lymphoblastic leukemia Phase 1
- Acute myeloid leukemia Phase 1
- Adenocarcinoma Phase 2
- Breast disorder Phase 1
- Breast ductal adenocarcinoma Phase 1
- Chordoma Phase 2
- Clear cell renal carcinoma Phase 2
- Colon carcinoma Phase 2
- COVID-19 Phase 2
- Dedifferentiated liposarcoma Phase 2
- Ductal breast carcinoma in situ Phase 2
- Endometrial cancer Phase 2
- Esophageal squamous cell carcinoma Phase 2
- Ewing sarcoma Phase 2
- Exocrine pancreatic carcinoma Phase 1
- Glioblastoma Phase 1
- Head and neck squamous cell carcinoma Phase 3
- Hepatocellular carcinoma Phase 2
- Hereditary breast ovarian cancer syndrome Phase 1
- Kidney disorder Phase 1
Other linked conditions (2)
- Childhood medulloblastoma
- Schizophrenia