Infigratinib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2021
- First approval year
- 2021
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Infigratinib
- Molecular weight
- 560.49
- Structure (SMILES)
- CCN1CCN(c2ccc(Nc3cc(N(C)C(=O)Nc4c(Cl)c(OC)cc(OC)c4Cl)ncn3)cc2)CC1
- bgj 398
- Bgj-398
- BGJ-398
- bgj398
- BGJ398
- BGJ398 (NVP-BGJ398)
- BGJ398 (NVP-BGJ398|INFIGRATINIB)
- bgj398 nvp bgj398
- bgj398 nvp bgj398 infigratinib
- infigratinib
- Infigratinib
- INFIGRATINIB
- INFIGRATINIB (BGJ398)
- infigratinib [INN]
- Infigratinib [MI]
- INFIGRATINIB [USAN]
- Infigratinib [WHO-DD]
- infigratinib bgj398
- infigratinib inn
- infigratinib mi
- infigratinib usan
- infigratinib who dd
- kin001 271
- KIN001-271
- mvp bgj398
And 7 more, listed on the interactive page.
- CAS registry numbers
- 872511-34-7
- ChEMBL ID
- CHEMBL1852688
- InChIKey
- QADPYRIHXKWUSV-UHFFFAOYSA-N
- PubChem compound IDs
- 53235510
- RxNorm IDs (RxCUI)
- 2550729
- FDA ingredient codes (UNII)
- A4055ME1VK
- L01E
- L01EN03
Sources for recorded values
- Applicant
- HELSINN HLTHCARE
- Approval date
- 28 May 2021
- Application number
- NDA214622
- Status
- application_withdrawn
- Status date
- 11 Oct 2022
- Approved indications
- Treatment of cholangiocarcinoma.
- Product number
- EMEA/H/C/005361
- Authorisation holder
- Helsinn Birex Pharmaceuticals Ltd
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Cholangiocarcinoma
European medicines record
- Patents
- 0
- Designations
- 5
- First in class
- No
- Fast track
- Yes
- Breakthrough designation
- No
- Orphan designation
- Yes
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- Yes
- Availability
- discontinued
- United States (FDA)
- Approved
- European Union (EMA)
- Application withdrawn
- Pharmacology name
- infigratinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- fibroblast growth factor receptor 1
- Gene symbol
- FGFR1
- Protein identifier
- P11362
- Median affinity
- 9.05
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- fibroblast growth factor receptor 2
- Gene symbol
- FGFR2
- Protein identifier
- P21802
- Median affinity
- 8.85
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- fibroblast growth factor receptor 4
- Gene symbol
- FGFR4
- Protein identifier
- P22455
- Median affinity
- 7.22
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- fibroblast growth factor receptor 3
- Gene symbol
- FGFR3
- Protein identifier
- P22607
- Median affinity
- 9
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- kinase insert domain receptor
- Gene symbol
- KDR
- Protein identifier
- P35968
- Median affinity
- 6.74
- Affinity units
- pIC50
- Mechanism
- Fibroblast growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Fibroblast growth factor receptor
- Protein identifier
- P11362
- Mechanism
- Fibroblast growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Fibroblast growth factor receptor
- Protein identifier
- P21802
- Mechanism
- Fibroblast growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Fibroblast growth factor receptor
- Protein identifier
- P22455
- Mechanism
- Fibroblast growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Fibroblast growth factor receptor
- Protein identifier
- P22607
Open Targets mechanisms
- Mechanism
- Fibroblast growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Fibroblast growth factor receptor
- Action type
- Inhibitor
- Gene symbol
- FGFR1
- Protein identifier
- P11362
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- FGFR2
- Protein identifier
- P21802
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- FGFR4
- Protein identifier
- P22455
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- FGFR3
- Protein identifier
- P22607
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- KDR
- Protein identifier
- P35968
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000181
- Subject identifier
- D002294
- Condition
- Glioblastoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000519
- Subject identifier
- D005909
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Melanoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000756
- Subject identifier
- D008545
- Condition
- Uterine Cervical Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001061
- Subject identifier
- D002583
- Condition
- Papillomavirus Infections
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001668
- Subject identifier
- D030361
- Condition
- Cholangiocarcinoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0005221
- Subject identifier
- D018281
- Condition
- Paraganglioma
- Highest recorded phase
- 2
- Condition identifier
- EFO:1000453
- Subject identifier
- D010235
- Condition
- Osteomalacia
- Highest recorded phase
- 2
- Condition identifier
- EFO:1002027
- Subject identifier
- D010018
- Condition
- Urinary Bladder Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0001187
- Subject identifier
- D001749
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0004992
- Subject identifier
- D009369
- Condition
- Achondroplasia
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0007037
- Subject identifier
- D000130
- Condition
- Breast Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0007254
- Subject identifier
- D001943
- Condition
- Gastrointestinal Stromal Tumors
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0011719
- Subject identifier
- D046152
- Condition
- Squamous Cell Carcinoma of Head and Neck
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0044704
- Subject identifier
- D000077195
- Condition identifier
- EFO_0000181
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000519
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0001668
- Highest recorded phase
- 2
- Condition identifier
- EFO_0005221
- Condition identifier
- EFO_1000453
- Highest recorded phase
- 2
- Condition identifier
- EFO_1002027
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0000448
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0001056
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0001187
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0001187
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0003210
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0003219
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004992
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005070
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005105
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005131
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005184
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005611
- Condition identifier
- MONDO_0007037
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0007254
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0007793
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0009831
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0010150
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0011719
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- Hydrogen bond acceptors
- 8
- Hydrogen bond donors
- 2
- Polar surface area
- 95.09
- Calculated partition coefficient (ALogP)
- 5.35
- Calculated partition coefficient (XLogP)
- 4.7
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 2
- Rotatable bonds
- 8
- Heavy atoms
- 38
- Molecular formula
- C26H31Cl2N7O3
- Monoisotopic mass
- 559.1865433
- Natural product
- Yes
- Recorded assays
- 1,551
- Active assays
- 226
- Confirmatory
- Other
- Antineoplastic Agents
Related records
Trials (30)
- A Dose Escalation Study in Adult Patients With Advanced Solid Malignancies
- A Phase 2 Study of BGJ398 in Patients With Recurrent GBM
- A Phase I Study of Oral BGJ398 in Asian Patients
- A Phase II, Single Arm Study of BGJ398 in Patients With Advanced Cholangiocarcinoma
- A Study to Evaluate the Efficacy and Safety of Infigratinib in Children and Adolescents With Achondroplasia
- An Interventional Study of Infigratinib in Children With Hypochondroplasia
- BGJ398 for Patients With Tumors With FGFR Genetic Alterations
- BGJ398 for the Treatment of Tumor-Induced Osteomalacia
- BGJ398 in Combination With Imatinib Mesylate in Patients With Untreated Advanced Gastrointestinal Stromal Tumor (GIST)
- BGJ398 in Non-Muscle-Invasive Urothelial Carcinoma of the Bladder
- BGJ398 in Treating Patients With FGFR Positive Recurrent Head and Neck Cancer
- Evaluation of Infigratinib in Patients With Locally Advanced or Metastatic Gastric Cancer or GEJ Adenocarcinoma
- Extension Study of Infigratinib in Children With Achondroplasia (ACH)
- Infigratinib Before Surgery for the Treatment of Upper Tract Urothelial Cancer
- Infigratinib for the Treatment of Advanced or Metastatic Solid Tumors in Patients With FGFR Gene Mutations
- Infigratinib in Recurrent High-Grade Glioma Patients
- Infigratinib in Subjects With GC or GEJ With FGFR2 Amplification or Other Solid Tumors With Other FGFR Alterations
- Interventional Study of Infigratinib in Children < 3 Years Old With Achondroplasia (ACH)
- LGX818 and MEK162 in Combination With a Third Agent (BKM120, LEE011, BGJ398 or INC280) in Advanced BRAF Melanoma
- Open-Label, Long-Term, Extension Study of Infigratinib in Children With Hypochondroplasia
Approved for (2)
In development for (25)
- Achondroplasia Phase 2
- Breast cancer Phase 1
- Cervical carcinoma Phase 1
- Cholangiocarcinoma Phase 3
- Gastric cancer Phase 2
- Gastroesophageal junction adenocarcinoma Phase 2
- Gastrointestinal stromal tumor Phase 1
- Glioblastoma Phase 2
- Glioma Phase 2
- Head and neck squamous cell carcinoma Phase 2
- Hematopoietic and lymphoid cell neoplasm Phase 2
- Human papilloma virus infection Phase 2
- Hypochondroplasia Phase 2
- Intrahepatic cholangiocarcinoma Phase 2
- Low grade glioma Phase 1
- Malignant pancreatic neoplasm Phase 1
- Melanoma Phase 2
- Oropharynx squamous cell carcinoma Phase 2
- Osteomalacia Phase 2
- Pancreatic ductal adenocarcinoma Phase 1
Other linked conditions (1)
- Bladder transitional cell carcinoma