Pyrotinib
Highest phase reached
Phase 3
Drug type
Small molecule
- Listing at source
- Listed
- Highest phase reached
- Phase 3
- Drug type
- Small molecule
- Drug name
- Pyrotinib
- Molecular weight
- 583.09
- Structure (SMILES)
- CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)/C=C/[C@H]1CCCN1C
- albumin bound paclitaxel trastuzumab pyrotinib
- capecitabine and pyrotinib
- dalpiciclib pyrotinib
- gq1001 pyrotinib
- her2 pyrotinib pertuzumab trastuzumab
- inetetamab pyrotinib nab paclitaxel
- palbociclib and exemestane plus trastuzumab and pyrotinib
- palbociclib trastuzumab pyrotinib and fulvestrant
- pyrotinib
- Pyrotinib
- Pyrotinib [WHO-DD]
- pyrotinib 240mg
- Pyrotinib 240mg
- pyrotinib 320mg
- Pyrotinib 320mg
- pyrotinib 400mg
- Pyrotinib 400mg
- pyrotinib and trastuzumab
- pyrotinib capecitabine bevacizumab
- pyrotinib maleate dalpiciclib trastuzumab letrozole
- pyrotinib maleate plus letrozole
- pyrotinib maleate shr6390 letrozole
- pyrotinib maleate tablets
- Pyrotinib Maleate Tablets
- pyrotinib maleate tablets nab paclitaxel
And 18 more, listed on the interactive page.
- CAS registry numbers
- 1269662-73-8
- ChEMBL ID
- CHEMBL3647420
- InChIKey
- SADXACCFNXBCFY-IYNHSRRRSA-N
- PubChem compound IDs
- 51039030
- FDA ingredient codes (UNII)
- CJN36EQM0H
- First in class
- No
- Orphan designation
- No
- Pharmacology name
- pyrotinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
- Mechanism
- Epidermal growth factor receptor erbB1 inhibitor
- Action type
- Inhibitor
- Target
- Epidermal growth factor receptor
- Protein identifier
- P00533
- Mechanism
- Receptor protein-tyrosine kinase erbB-2 inhibitor
- Action type
- Inhibitor
- Target
- Receptor tyrosine-protein kinase erbB-2
- Protein identifier
- P04626
- Action
- Irreversible inhibition
- Action type
- IRREVERSIBLE_INHIBITION
- Target
- epidermal growth factor receptor
- Gene symbol
- EGFR
- Protein identifier
- P00533
- Median affinity
- 7.89
- Affinity units
- pIC50
- Action
- Irreversible inhibition
- Action type
- IRREVERSIBLE_INHIBITION
- Target
- erb-b2 receptor tyrosine kinase 2
- Gene symbol
- ERBB2
- Protein identifier
- P04626
- Median affinity
- 7.42
- Affinity units
- pIC50
- Mechanism
- Epidermal growth factor receptor erbB1 inhibitor
- Action type
- Inhibitor
- Target
- Epidermal growth factor receptor
- Mechanism
- Receptor protein-tyrosine kinase erbB-2 inhibitor
- Action type
- Inhibitor
- Target
- Receptor tyrosine-protein kinase erbB-2
- Condition
- Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Breast Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003869
- Subject identifier
- D001943
- Condition
- Triple Negative Breast Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005537
- Subject identifier
- D064726
- Condition
- Digestive System Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0008549
- Subject identifier
- D004067
- Condition
- Stomach Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0001056
- Subject identifier
- D013274
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0005575
- Subject identifier
- D015179
- Condition
- Breast Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0007254
- Subject identifier
- D001943
- Condition identifier
- EFO_0000616
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 3
- Condition identifier
- EFO_0003869
- Highest recorded phase
- 2
- Condition identifier
- EFO_0005922
- Highest recorded phase
- 2
- Condition identifier
- EFO_0008549
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000294
- Condition identifier
- MONDO_0000521
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0001056
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0003060
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004379
- Condition identifier
- MONDO_0004669
- Condition identifier
- MONDO_0004950
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0004992
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005028
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005061
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005233
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005494
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005575
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005580
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0007254
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0007256
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0008903
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0009831
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0021040
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0040679
- Highest recorded phase
- 2
- Event
- alanine aminotransferase increased
- Reports
- 9
- Reporting signal score
- 24.5059
- Event
- anaemia
- Reports
- 12
- Reporting signal score
- 25.5811
- Event
- aspartate aminotransferase increased
- Reports
- 8
- Reporting signal score
- 21.6817
- Event
- blood bilirubin increased
- Reports
- 3
- Reporting signal score
- 8.87439
- Event
- decreased appetite
- Reports
- 5
- Reporting signal score
- 10.1523
- Event
- diarrhoea
- Reports
- 19
- Reporting signal score
- 35.2218
- Event
- drug resistance
- Reports
- 4
- Reporting signal score
- 11.5473
- Event
- fatigue
- Reports
- 7
- Reporting signal score
- 8.31454
- Event
- granulocyte count decreased
- Reports
- 2
- Reporting signal score
- 10.3622
- Event
- hepatic function abnormal
- Reports
- 4
- Reporting signal score
- 10.245
- Event
- hypokalaemia
- Reports
- 6
- Reporting signal score
- 16.2658
- Event
- leukopenia
- Reports
- 6
- Reporting signal score
- 15.2867
- Event
- metastasis
- Reports
- 5
- Reporting signal score
- 24.1175
- Event
- mouth ulceration
- Reports
- 3
- Reporting signal score
- 8.40937
- Event
- myelosuppression
- Reports
- 12
- Reporting signal score
- 58.5585
- Event
- nausea
- Reports
- 13
- Reporting signal score
- 16.0045
- Event
- neutropenia
- Reports
- 10
- Reporting signal score
- 22.1075
- Event
- neutrophil count decreased
- Reports
- 3
- Reporting signal score
- 7.97058
- Event
- palmar-plantar erythrodysaesthesia syndrome
- Reports
- 9
- Reporting signal score
- 34.3669
- Event
- pigmentation disorder
- Reports
- 3
- Reporting signal score
- 13.1924
- Event
- rash
- Reports
- 6
- Reporting signal score
- 8.2457
- Event
- stomatitis
- Reports
- 6
- Reporting signal score
- 16.5146
- Event
- thrombocytopenia
- Reports
- 8
- Reporting signal score
- 16.608
- Event
- transaminases increased
- Reports
- 3
- Reporting signal score
- 8.74789
- Event
- vomiting
- Reports
- 12
- Reporting signal score
- 18.4451
- NCT01937689
- NCT02361112
- NCT02422199
- NCT02500199
- NCT02973737
- NCT03080805
- NCT03412383
- NCT03588091
- NCT03691051
- NCT03735966
- NCT03772353
- NCT03863223
- NCT03876587
- NCT03923166
- NCT03923179
- NCT03980054
- NCT03993964
- NCT03997539
- NCT04001621
- NCT04033172
- NCT04034589
- NCT04066790
- NCT04088110
- NCT04095390
- NCT04126525
And 82 more, listed on the interactive page.
- Hydrogen bond acceptors
- 8
- Hydrogen bond donors
- 2
- Polar surface area
- 112.4
- Calculated partition coefficient (ALogP)
- 6.47
- Calculated partition coefficient (XLogP)
- 5.4
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 2
- Rotatable bonds
- 10
- Heavy atoms
- 42
- Molecular formula
- C32H31ClN6O3
- Monoisotopic mass
- 582.2146166
- Natural product
- No
- Recorded assays
- 33
- Active assays
- 29
- Confirmatory
- Other
Related records
Trials (170)
- 18F-FDG Uptake Heterogeneity Predicts Pyrotinib Response
- A Clinica Study of Pyrotinib in Patients of Advanced Non-Small Cell Lung Cancer With HER2 Mutation
- A Clinical Study of JS105 in Combination With Other Anti-tumor Therapies in Patients With Solid Tumors
- A Clinical Study of Pyrotinib in Patients With HER2-positive Advanced Colorectal Cancer
- A Drug-drug Interaction Trial of Loperamide Pharmacokinetics Effect on Pyrotinib Maleate
- A Phase II Clinical Study of Treatment With Disitamb Vedotin Plus Pyrotinib in HER2-positive Early Breast Cancer
- A Phase II Study of Trastuzumab Deruxtecan (T-DXd) Plus Pyrotinib in HER2-Positive Advanced Breast Cancer After Progression on T-DXd
- A Phase Ⅱ Trial of Pyrotinib Combination With CDK4/6 Inhibitor SHR6390 in Patients Prior Trastuzumab-treated Advanced HER2-Positive Breast Cancer
- A Prospective, Open-label, Exploratory Basket Trial to Evaluate the Efficacy and Safety of Sintilimab Combined With Pyrotinib ± Chemotherapy in Patients With Advanced Digestive System Tumors
- A Prospective, Open, Multicenter Single-arm Clinical Studie of Docetaxel, Carboplatin Combined With Inetetamab and Pyrotinib in the Treatment of Local-advanced HER2-positive Breast Cancer
- A Real-World Study of Pyrotinib Maleate in the Treatment of Advanced/Metastatic Non-Small Cell Lung Cancer With Rare Mutations in HER2
- A Study of ARX788 Combined With Pyrotinib Maleate Versus TCBHP (Trastuzumab Plus Pertuzumab With Docetaxel and Carboplatin) as Neoadjuvant Treatment in HER2-positive Breast Cancer Patients
- A Study of Diarrhea and Intestinal Flora Changes Caused by Pyrotinib in Breast Cancer
- A Study of Evaluating The Effects Of Pyrotinib After Adjuvant Trastuzumab In Women With Early Stage Breast Cancer
- A Study of Neoadjuvant SHR6390 in Combination With Anastrozole, Pyrotinib, and Trastuzumab in Patients With ER+/HER2+ Breast Cancer.
- A Study of Pyrotinib Combined With Capecitabine for Metastatic HER-2 Positive Colorectal Cancer
- A Study of Pyrotinib in Combination With Trastuzumab and Docetaxel in Patients With HER2 Metastatic Breast Cancer
- A Study of Pyrotinib Plus Capecitabine in Patients With Brain Metastases From HER2-positive Metastatic Breast Cancer
- A Study of Pyrotinib Plus Capecitabine in Patients With HER2+ Metastatic Breast Cancer
- A Study of Pyrotinib Plus Capecitabine Versus Lapatinib Plus Capecitabine in Patients With HER2+Metastatic Breast Cancer Who Have Prior Received Anthracyclin, Taxane or Trastuzumab
In development for (20)
- Biliary tract cancer Phase 2
- Breast cancer Phase 3
- Breast neoplasm Phase 3
- Cancer Phase 2
- Colorectal cancer Phase 2
- Digestive system neoplasm Phase 2
- Esophageal adenocarcinoma Phase 2
- Esophageal squamous cell carcinoma Phase 2
- Gastric cancer Phase 2
- Gastric carcinoma Phase 1
- Hepatocellular carcinoma Phase 2
- Lung adenocarcinoma Phase 2
- Lung cancer Phase 2
- Malignant pancreatic neoplasm Phase 2
- Neoplasm Phase 2
- Non-small cell lung carcinoma Phase 3
- Pancreatic neoplasm Phase 2
- Salivary gland carcinoma Phase 2
- Triple-negative breast carcinoma Phase 2
- Urothelial carcinoma Phase 2
Other linked conditions (3)
- Female breast carcinoma
- HER2 positive breast carcinoma
- Salivary gland cancer