Fruquintinib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2023
- First approval year
- 2023
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Fruquintinib
- Molecular weight
- 393.4
- Structure (SMILES)
- CNC(=O)c1c(C)oc2cc(Oc3ncnc4cc(OC)c(OC)cc34)ccc12
- fruzaqla
- Fruzaqla
- camrelizumab fruquintinib
- fruquintinib
- Fruquintinib
- FRUQUINTINIB
- Fruquintinib (HMPL-013)
- fruquintinib [INN]
- Fruquintinib [MI]
- FRUQUINTINIB [USAN]
- Fruquintinib [WHO-DD]
- Fruquintinib Capsules
- fruquintinib inn
- fruquintinib mi
- fruquintinib usan
- fruquintinib who dd
- hmpl 013
- Hmpl-013
- HMPL-013
- hmpl013
- HMPL013
- Standard of care (Fruquintinib)
- Targeted Therapy Agent (Fruquintinib)
- CAS registry numbers
- 1194506-26-7
- ChEMBL ID
- CHEMBL4303214
- InChIKey
- BALLNEJQLSTPIO-UHFFFAOYSA-N
- PubChem compound IDs
- 44480399
- RxNorm IDs (RxCUI)
- 2670179
- FDA ingredient codes (UNII)
- 49DXG3M5ZW
- L01EK
- L01EK04
Sources for recorded values
- Applicant
- TAKEDA PHARMS USA
- Approval date
- 8 Nov 2023
- Application number
- NDA217564
- Status
- Authorised
- Status date
- 20 Jun 2024
- Authorisation date
- 20 Jun 2024
- Approved indications
- Fruzaqla as monotherapy is indicated for the treatment of adult patients with metastatic colorectal cancer (mCRC) who have been previously treated with available standard therapies, including fluoropyrimidine-, oxaliplatin-, and irinotecan based chemotherapies, anti VEGF agents, and anti EGFR agents, and who have progressed on or are intolerant to treatment with either trifluridine tipiracil or regorafenib.
- Product number
- EMEA/H/C/005979
- Authorisation holder
- Takeda Pharmaceuticals International AG Ireland
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- Yes
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Colorectal Neoplasms
European medicines record
- Patents
- 4
- Designations
- 2
- Earliest recorded loss of exclusivity
- 7 Sept 2035
- First in class
- No
- Fast track
- Yes
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Pharmacology name
- fruquintinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- fms related receptor tyrosine kinase 1
- Gene symbol
- FLT1
- Protein identifier
- P17948
- Median affinity
- 7.48
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- fms related receptor tyrosine kinase 4
- Gene symbol
- FLT4
- Protein identifier
- P35916
- Median affinity
- 9.3
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- kinase insert domain receptor
- Gene symbol
- KDR
- Protein identifier
- P35968
- Median affinity
- 7.6
- Affinity units
- pIC50
- Primary target
- Yes
- Mechanism
- Vascular endothelial growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor
- Protein identifier
- P17948
- Mechanism
- Vascular endothelial growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor
- Protein identifier
- P35916
- Mechanism
- Vascular endothelial growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor
- Protein identifier
- P35968
Open Targets mechanisms
- Mechanism
- Vascular endothelial growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor
- Condition
- Carcinoma, Hepatocellular
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000182
- Subject identifier
- D006528
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000365
- Subject identifier
- D015179
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000681
- Subject identifier
- D002292
- Condition
- Liver Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001421
- Subject identifier
- D008107
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002618
- Subject identifier
- D010190
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Kidney Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003086
- Subject identifier
- D007674
- Condition
- Stomach Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003897
- Subject identifier
- D013274
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0004142
- Subject identifier
- D015179
- Condition
- Esophageal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005922
- Subject identifier
- D004938
- Condition
- Rectal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:1000657
- Subject identifier
- D012004
- Condition
- Sarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:1001968
- Subject identifier
- D012509
- Condition
- Stomach Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0001056
- Subject identifier
- D013274
- Condition
- Adenocarcinoma
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0003219
- Subject identifier
- D000230
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0004992
- Subject identifier
- D009369
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0005575
- Subject identifier
- D015179
- Condition
- Breast Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0007254
- Subject identifier
- D001943
- Condition
- Lung Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0008903
- Subject identifier
- D008175
- Condition
- Endometrial Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0011962
- Subject identifier
- D016889
- Condition
- Colonic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0021063
- Subject identifier
- D003110
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000681
- Condition identifier
- EFO_0000756
- Condition identifier
- EFO_0001421
- Highest recorded phase
- 1
- Condition identifier
- EFO_0002618
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 3
- Condition identifier
- EFO_0003086
- Highest recorded phase
- 1
- Condition identifier
- EFO_0003897
- Condition identifier
- EFO_0004142
- Condition identifier
- EFO_0005922
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000657
- Condition identifier
- EFO_1001480
- Highest recorded phase
- 2
- Condition identifier
- EFO_1001480
- Highest recorded phase
- 3
- Condition identifier
- EFO_1001951
- Highest recorded phase
- 2
- Condition identifier
- EFO_1001968
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0001056
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0002691
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0003060
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0003219
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0003219
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0004992
- Condition identifier
- MONDO_0004992
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005005
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005008
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005036
- Highest recorded phase
- 3
And 29 more, listed on the interactive page.
- Event
- colorectal cancer recurrent
- Reports
- 1
- Reporting signal score
- 8.56296
- Event
- hyperplastic cholecystopathy
- Reports
- 1
- Reporting signal score
- 8.33057
- Event
- milia
- Reports
- 1
- Reporting signal score
- 7.8767
- Event
- proteinuria
- Reports
- 2
- Reporting signal score
- 7.9142
- Event
- rash
- Reports
- 4
- Reporting signal score
- 8.09473
- Event
- thymus disorder
- Reports
- 1
- Reporting signal score
- 8.02187
- Event
- thymus enlargement
- Reports
- 1
- Reporting signal score
- 7.9911
- NCT01645215
- NCT03903705
- NCT04577963
- NCT04716634
- NCT01975077
- NCT02196688
- NCT02314819
- NCT04179084
- NCT04296019
- NCT04695470
- NCT04733963
- NCT05025631
- NCT05435313
- NCT05451719
- NCT05511051
- NCT05771181
- NCT05954429
- NCT06010888
- NCT06168786
- NCT06199973
- NCT06218888
- NCT06356597
- NCT06441565
- NCT02415023
- NCT05177068
And 36 more, listed on the interactive page.
- Dose
- 5 mg
- Route
- Oral
- How often
- Once daily
- Swallow capsule whole
- Take with or without food
- Hydrogen bond acceptors
- 7
- Hydrogen bond donors
- 1
- Polar surface area
- 95.71
- Calculated partition coefficient (ALogP)
- 3.85
- Calculated partition coefficient (XLogP)
- 3.4
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 5
- Heavy atoms
- 29
- Molecular formula
- C21H19N3O5
- Monoisotopic mass
- 393.13247072
- Natural product
- Yes
- 63020-210
- 63020-225
- Recorded assays
- 246
- Active assays
- 17
- Confirmatory
- Other
- Tyrosine Kinase Inhibitors
- Antineoplastic Agents
Related records
Trials (166)
- - IKF/AIO-QUINTIS - Evaluating Fruquintinib in Combination With Tislelizumab in Microsatellite Stable / Proficient Mismatch Repair (MSS/pMMR) Metastatic Colorectal Cancer Without Active Liver Metastases
- : A Phase Ib/II Study To Evaluate Fruquintinib Monotherapy Or Plus Sintilimab In Advanced Solid Tumors
- A Clinical Study of Iparomlimab and Tuvonralimab Combined With Fruquintinib and Heterogeneous Radiotherapy Versus Fruquintinib as Third-Line and Subsequent-Line Treatment for Metastatic Colorectal Cancer
- A Clinical Study on the Efficacy and Safety of Fruquintinib in Combination With PD-1 Monoclonal Antibody and Chidamide in Refractory MSS Metastatic Colorectal Cancer
- A Clinical Study to Evaluate Injection TQB2102 for the Treatment of Patients With HER2 IHC3+ Advanced Colorectal Cancer Who Progressed After Treatment With Oxaliplatin, Irinotecan and Fluoropyrimidine-Based Drugs
- A Clinical Trial of Fruquintinib in Patients With Advanced Non-small Cell Lung Cancer
- A Mass Balance Study to Investigate the Absorption, Metabolism, and Excretion Of [14C] Fruquintinib
- A Multi-Center, Open-Label Study of Fruquintinib in Solid Tumors and Colorectal, and Breast Cancers
- A Multicenter, Phase Ib/II Clinical Trial to Evaluate the Efficacy and Safety of Concurrent Combination Therapy of S-531011 Plus Fruquintinib or S-531011 Plus Fruquintinib Plus Pembrolizumab in Patients With MSS/pMMR Colorectal Cancer
- A Phase 1-2 of ST316 With Selected Advanced Unresectable and Metastatic Solid Tumors
- A Phase 2 Trial of Fruquintinib and Tislelizumab in ctDNA-defined Minimal Residual Disease in Colorectal Cancer After Completion of Adjuvant Chemotherapy
- A Phase Ib Study of Fruquintinib in 3rd Line mCRC
- A Phase Ib/2 Clinical Study of Fruquintinib Combined With Paclitaxel in the Treatment of Advanced Gastric Cancer
- A Phase Ib/II Clinical Study of LBL-024 Combination Therapy in Patients With Metastatic Colorectal Carcinoma
- A Phase Ib/II Study of HDM2017 in Combination With Standard of Care in Advanced Colorectal Cancer
- A Phase II Clinical Study of Aipalolitovorelizumab (QL1706) Combined With Fruquintinib in the Treatment of Immunodominant pMMR/MSS Metastatic Colorectal Cancer That Has Failed Second-line or Above Treatment
- A Phase II Clinical Study of Fruquintinib Combined With RC48 in the Treatment of Previously Treated HER2-positive Locally Advanced or Metastatic Gastric or Gastroesophageal Junction (G/GEJ) Cancer
- A Phase II Clinical Study of Fruquintinib Combined With S-1 for Advanced Esophageal Squamous Cell Carcinoma
- A Phase II Clinical Study of the Efficacy and Safety of Tislelizumab Combined With Fruquintinib and Chidamide in the Treatment of Unresectable or Advanced Microsatellite Stabilized (MSS/pMMR) Colorectal Cancer With Liver Metastases
- A Phase II Clinical Trial of Fruquintinib as Third Line Treatment in Advanced Pancreatic Cancer
Approved for (5)
In development for (17)
- Breast cancer Phase 1
- Colorectal carcinoma Phase 2
- Endometrial cancer Phase 1
- Esophageal squamous cell carcinoma Phase 2
- Exocrine pancreatic carcinoma Phase 2
- Gastric cancer Phase 3
- Gastric neoplasm Phase 3
- Gastroesophageal junction adenocarcinoma Phase 1
- Hepatocellular carcinoma Phase 2
- Kidney disorder Phase 1
- Liver disorder Phase 1
- Lung cancer Phase 2
- Malignant colon neoplasm Phase 2
- Non-small cell lung carcinoma Phase 3
- Rectal cancer Phase 2
- Renal cell carcinoma Phase 2
- Soft tissue sarcoma Phase 2
Other linked conditions (2)
- Melanoma
- Nonpapillary renal cell carcinoma