> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/regorafenib-333c1c36-b89a-41d5-b39e-bcec7346fe94
> Record changed: 2026-10-13

# Regorafenib

Highest phase reached

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1946170)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1946170)

First approval year

2012

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1946170)

## Development status

**First approval year**

2012

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1946170)

**Listing at source**

Listed

**Highest phase reached**

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1946170)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1946170)

**Drug name**

Regorafenib

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1946170)

**Molecular weight**

482.82

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1946170)

**Structure (SMILES)**

CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)c(F)c2)ccn1

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1946170)

### Brand names (2)

- stivarga
- Stivarga

### Other names (39)

- bay 73 4506
- bay 73 4506 monohydrate
- BAY 73-4506
- BAY 73-4506 monohydrate
- bay 734506
- bay 734506 monohydrate
- BAY-73-4506
- BAY-73-4506 MONOHYDRATE
- BAY-734506
- BAY-734506 MONOHYDRATE
- cadonilimab regorafenib
- regorafenib
- Regorafenib
- Regorafenib (BAY 73-4506)
- Regorafenib (BAY73-4506)
- Regorafenib (CT)
- Regorafenib (Stivarga)
- regorafenib \[INN\]
- REGORAFENIB \[MI\]
- REGORAFENIB \[VANDF\]
- Regorafenib \[WHO-DD\]
- Regorafenib 160 mg
- Regorafenib 20MG
- Regorafenib 30 mg capsules
- Regorafenib 30 MG Oral Tablet

And 14 more, listed on the interactive page.

## Identifiers

**ATC classification codes**

- L01EX05

Sources for recorded values

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1946170)

**CAS registry numbers**

- 755037-03-7

**ChEMBL ID**

CHEMBL1946170

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1946170)

**InChIKey**

FNHKPVJBJVTLMP-UHFFFAOYSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1946170)

**PubChem compound IDs**

- 11167602

**RxNorm IDs (RxCUI)**

- 1312397

**FDA ingredient codes (UNII)**

- 24T2A1DOYB

## Regulatory information

### United States

**Applicant**

BAYER HLTHCARE

**Approval date**

27 Sept 2012

**Application number**

NDA203085

### European Union

**Status**

Authorised

**Status date**

26 Aug 2013

**Authorisation date**

26 Aug 2013

**Approved indications**

Stivarga is indicated as monotherapy for the treatment of adult patients with: metastatic colorectal cancer (CRC) who have been previously treated with, or are not considered candidates for, available therapies - these include fluoropyrimidine-based chemotherapy, an anti-VEGF therapy and an anti-EGFR therapy; unresectable or metastatic gastrointestinal stromal tumors (GIST) who progressed on or are intolerant to prior treatment with imatinib and sunitinib; hepatocellular carcinoma (HCC) who have been previously treated with sorafenib.

**Product number**

EMEA/H/C/002573

**Authorisation holder**

Bayer Pharma AG

**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

- Colorectal Neoplasms

European medicines record

Source: [www.ema.europa.eu](https://www.ema.europa.eu/en/medicines/human/EPAR/stivarga)

### Other regulatory facts

**Patents**

4

**Designations**

4

**Earliest recorded loss of exclusivity**

9 Jul 2032

**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

**Boxed warning**

Yes

## Pharmacology

### Drug classification

**Pharmacology name**

regorafenib

**Type**

Synthetic organic

**Drug name stem**

\-rafenib

**Approval recorded by Guide to Pharmacology**

Yes

#### Administration routes

- Oral

### Mechanisms of action (20)

- **Action**  
Inhibition

**Action type**  
Inhibitor

**Target**  
B-Raf proto-oncogene, serine/threonine kinase

**Gene symbol**  
BRAF

**Protein identifier**  
P15056

**Median affinity**

7.55

**Affinity units**  
pIC50

**Primary target**  
Yes
- **Action**  
Inhibition

**Action type**  
Inhibitor

**Target**  
kinase insert domain receptor

**Gene symbol**  
KDR

**Protein identifier**  
P35968

**Median affinity**

7.9

**Affinity units**  
pIC50
- **Mechanism**  
Discoidin domain-containing receptor 2 inhibitor

**Action type**  
Inhibitor

**Target**  
Discoidin domain-containing receptor 2

**Protein identifier**  
Q16832
- **Mechanism**  
Ephrin type-A receptor 2 inhibitor

**Action type**  
Inhibitor

**Target**  
Ephrin type-A receptor 2

**Protein identifier**  
P29317
- **Mechanism**  
Fibroblast growth factor receptor 1 inhibitor

**Action type**  
Inhibitor

**Target**  
Fibroblast growth factor receptor 1

**Protein identifier**  
P11362
- **Mechanism**  
Fibroblast growth factor receptor 2 inhibitor

**Action type**  
Inhibitor

**Target**  
Fibroblast growth factor receptor 2

**Protein identifier**  
P21802
- **Mechanism**  
MAP kinase p38 beta inhibitor

**Action type**  
Inhibitor

**Target**  
Mitogen-activated protein kinase 11

**Protein identifier**  
Q15759
- **Mechanism**  
Nerve growth factor receptor Trk-A inhibitor

**Action type**  
Inhibitor

**Target**  
High affinity nerve growth factor receptor

**Protein identifier**  
P04629
- **Mechanism**  
Platelet-derived growth factor receptor inhibitor

**Action type**  
Inhibitor

**Target**  
Platelet-derived growth factor receptor

**Protein identifier**  
P09619
- **Mechanism**  
Platelet-derived growth factor receptor inhibitor

**Action type**  
Inhibitor

**Target**  
Platelet-derived growth factor receptor

**Protein identifier**  
P16234
- **Mechanism**  
Serine/threonine-protein kinase B-raf inhibitor

**Action type**  
Inhibitor

**Target**  
Serine/threonine-protein kinase B-raf

**Protein identifier**  
P15056
- **Mechanism**  
Serine/threonine-protein kinase RAF inhibitor

**Action type**  
Inhibitor

**Target**  
RAF proto-oncogene serine/threonine-protein kinase

**Protein identifier**  
P04049
- **Mechanism**  
Stem cell growth factor receptor inhibitor

**Action type**  
Inhibitor

**Target**  
Mast/stem cell growth factor receptor Kit

**Protein identifier**  
P10721
- **Mechanism**  
Tyrosine-protein kinase ABL inhibitor

**Action type**  
Inhibitor

**Target**  
Tyrosine-protein kinase ABL1

**Protein identifier**  
P00519
- **Mechanism**  
Tyrosine-protein kinase FRK inhibitor

**Action type**  
Inhibitor

**Target**  
Tyrosine-protein kinase FRK

**Protein identifier**  
P42685
- **Mechanism**  
Tyrosine-protein kinase receptor RET inhibitor

**Action type**  
Inhibitor

**Target**  
Proto-oncogene tyrosine-protein kinase receptor Ret

**Protein identifier**  
P07949
- **Mechanism**  
Tyrosine-protein kinase TIE-2 inhibitor

**Action type**  
Inhibitor

**Target**  
Angiopoietin-1 receptor

**Protein identifier**  
Q02763
- **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 (15)

- **Mechanism**  
Discoidin domain-containing receptor 2 inhibitor

**Action type**  
Inhibitor

**Target**  
Discoidin domain-containing receptor 2
- **Mechanism**  
Ephrin type-A receptor 2 inhibitor

**Action type**  
Inhibitor

**Target**  
Ephrin type-A receptor 2
- **Mechanism**  
Fibroblast growth factor receptor 1 inhibitor

**Action type**  
Inhibitor

**Target**  
Fibroblast growth factor receptor 1
- **Mechanism**  
Fibroblast growth factor receptor 2 inhibitor

**Action type**  
Inhibitor

**Target**  
Fibroblast growth factor receptor 2
- **Mechanism**  
MAP kinase p38 beta inhibitor

**Action type**  
Inhibitor

**Target**  
Mitogen-activated protein kinase 11
- **Mechanism**  
Nerve growth factor receptor Trk-A inhibitor

**Action type**  
Inhibitor

**Target**  
High affinity nerve growth factor receptor
- **Mechanism**  
Platelet-derived growth factor receptor inhibitor

**Action type**  
Inhibitor

**Target**  
Platelet-derived growth factor receptor
- **Mechanism**  
Serine/threonine-protein kinase B-raf inhibitor

**Action type**  
Inhibitor

**Target**  
Serine/threonine-protein kinase B-raf
- **Mechanism**  
Serine/threonine-protein kinase RAF inhibitor

**Action type**  
Inhibitor

**Target**  
RAF proto-oncogene serine/threonine-protein kinase
- **Mechanism**  
Stem cell growth factor receptor inhibitor

**Action type**  
Inhibitor

**Target**  
Mast/stem cell growth factor receptor Kit
- **Mechanism**  
Tyrosine-protein kinase ABL inhibitor

**Action type**  
Inhibitor

**Target**  
Tyrosine-protein kinase ABL1
- **Mechanism**  
Tyrosine-protein kinase FRK inhibitor

**Action type**  
Inhibitor

**Target**  
Tyrosine-protein kinase FRK
- **Mechanism**  
Tyrosine-protein kinase receptor RET inhibitor

**Action type**  
Inhibitor

**Target**  
Proto-oncogene tyrosine-protein kinase receptor Ret
- **Mechanism**  
Tyrosine-protein kinase TIE-2 inhibitor

**Action type**  
Inhibitor

**Target**  
Angiopoietin-1 receptor
- **Mechanism**  
Vascular endothelial growth factor receptor inhibitor

**Action type**  
Inhibitor

**Target**  
Vascular endothelial growth factor receptor

### DrugCentral mechanisms (3)

- **Action type**  
Inhibitor

**Gene symbol**  
BRAF

**Protein identifier**  
P15056

**Organism**  
Homo sapiens

**Target development level**  
Clinical
- **Action type**  
Inhibitor

**Gene symbol**  
EPHX2

**Protein identifier**  
P34913

**Organism**  
Homo sapiens

**Target development level**  
Chemical evidence
- **Action type**  
Inhibitor

**Gene symbol**  
KDR

**Protein identifier**  
P35968

**Organism**  
Homo sapiens

**Target development level**  
Clinical

### Investigated indications (41)

- **Condition**  
Carcinoma, Hepatocellular

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000182

**Subject identifier**  
D006528
- **Condition**  
Myelodysplastic Syndromes

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0000198

**Subject identifier**  
D009190
- **Condition**  
Leukemia, Myeloid, Acute

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0000222

**Subject identifier**  
D015470
- **Condition**  
Carcinoma, Adenoid Cystic

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000231

**Subject identifier**  
D003528
- **Condition**  
Colorectal Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
EFO:0000365

**Subject identifier**  
D015179
- **Condition**  
Melanoma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000389

**Subject identifier**  
D008545
- **Condition**  
Glioblastoma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000519

**Subject identifier**  
D005909
- **Condition**  
Liposarcoma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000569

**Subject identifier**  
D008080
- **Condition**  
Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
EFO:0000616

**Subject identifier**  
D009369
- **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**  
2

**Condition identifier**  
EFO:0000691

**Subject identifier**  
D012509
- **Condition**  
Small Cell Lung Carcinoma

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0000702

**Subject identifier**  
D055752
- **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**  
Pancreatic Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0002618

**Subject identifier**  
D010190
- **Condition**  
Rhabdomyosarcoma

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0002918

**Subject identifier**  
D012208
- **Condition**  
Ovarian Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0003893

**Subject identifier**  
D010051
- **Condition**  
Hemangiosarcoma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0003968

**Subject identifier**  
D006394
- **Condition**  
Colorectal Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
EFO:0004142

**Subject identifier**  
D015179
- **Condition**  
Cholangiocarcinoma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0005221

**Subject identifier**  
D018281
- **Condition**  
Bile Duct Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0005540

**Subject identifier**  
D001650
- **Condition**  
Macular Degeneration

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0009606

**Subject identifier**  
D008268
- **Condition**  
Bone Neoplasms

**Highest recorded phase**  
1

**Condition identifier**  
EFO:1000350

**Subject identifier**  
D001859
- **Condition**  
Rectal Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:1000657

**Subject identifier**  
D012004

And 16 more, listed on the interactive page.

### Open Targets indications (102)

- **Condition identifier**  
EFO\_0000174

**Highest recorded phase**  
1
- **Condition identifier**  
EFO\_0000182

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0000222

**Highest recorded phase**  
1
- **Condition identifier**  
EFO\_0000231

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000365
- **Condition identifier**  
EFO\_0000519

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000616
- **Condition identifier**  
EFO\_0000637

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000681

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000691

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000756

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0002618

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0003893

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0003968

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0004142
- **Condition identifier**  
EFO\_0004920

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0005221

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0005540

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_1000657

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_1001480
- **Condition identifier**  
EFO\_1001480

**Highest recorded phase**  
4
- **Condition identifier**  
EFO\_1001513
- **Condition identifier**  
EFO\_1001949

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_1001951

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_1001961

**Highest recorded phase**  
2

And 77 more, listed on the interactive page.

### Warnings

- **Warning**  
Black Box Warning

**Effect**  
hepatotoxicity

### Open Targets warnings

- **Warning**  
Black Box Warning

**Effect**  
hepatotoxicity

**Country**  
United States

### Reported adverse events (49)

- **Event**  
abdominal pain

**Reports**  
244

**Reporting signal score**

138.351
- **Event**  
abdominal pain upper

**Reports**  
169

**Reporting signal score**

111.216
- **Event**  
alpha 1 foetoprotein increased

**Reports**  
19

**Reporting signal score**

62.0471
- **Event**  
ascites

**Reports**  
86

**Reporting signal score**

115.348
- **Event**  
asthenia

**Reports**  
421

**Reporting signal score**

326.333
- **Event**  
back pain

**Reports**  
146

**Reporting signal score**

58.1083
- **Event**  
blister

**Reports**  
223

**Reporting signal score**

426.451
- **Event**  
blood bilirubin increased

**Reports**  
116

**Reporting signal score**

171.666
- **Event**  
blood pressure increased

**Reports**  
210

**Reporting signal score**

224.476
- **Event**  
carcinoembryonic antigen increased

**Reports**  
60

**Reporting signal score**

219.337
- **Event**  
colon cancer

**Reports**  
99

**Reporting signal score**

237.101
- **Event**  
colon cancer metastatic

**Reports**  
24

**Reporting signal score**

78.6843
- **Event**  
colorectal cancer

**Reports**  
119

**Reporting signal score**

512.941
- **Event**  
colorectal cancer metastatic

**Reports**  
132

**Reporting signal score**

632.47
- **Event**  
constipation

**Reports**  
205

**Reporting signal score**

137.61
- **Event**  
decreased appetite

**Reports**  
544

**Reporting signal score**

846.707
- **Event**  
dehydration

**Reports**  
237

**Reporting signal score**

229.793
- **Event**  
diarrhoea

**Reports**  
690

**Reporting signal score**

495.439
- **Event**  
dry mouth

**Reports**  
93

**Reporting signal score**

89.8488
- **Event**  
dry skin

**Reports**  
141

**Reporting signal score**

212.403
- **Event**  
dysphonia

**Reports**  
437

**Reporting signal score**  
1,131.24
- **Event**  
erythema

**Reports**  
159

**Reporting signal score**

90.1444
- **Event**  
exercise tolerance decreased

**Reports**  
33

**Reporting signal score**

70.117
- **Event**  
fatigue

**Reports**  
836

**Reporting signal score**

693.921
- **Event**  
gait disturbance

**Reports**  
137

**Reporting signal score**

76.7402

And 24 more, listed on the interactive page.

### Trial references (143)

- NCT00664326  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00664326)
- NCT00934882  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00934882)
- NCT01289821  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01289821)
- NCT01584830  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01584830)
- NCT01939223  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01939223)
- NCT02096354  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02096354)
- NCT02195011  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02195011)
- NCT02465502  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02465502)
- NCT04776148  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04776148)
- NCT05328908  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05328908)
- NCT05426811  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05426811)
- NCT00960258  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00960258)
- NCT01096030  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01096030)
- NCT01117623  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01117623)
- NCT01287598  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01287598)
- NCT01322438  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01322438)
- NCT01339104  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01339104)
- NCT01853046  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01853046)
- NCT01973868  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01973868)
- NCT02001909  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02001909)
- NCT02106845  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02106845)
- NCT02168777  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02168777)
- NCT02466802  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02466802)
- NCT02925234  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02925234)
- NCT03406871  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03406871)

And 118 more, listed on the interactive page.

## Dosing

**Dose**

160 mg

**Route**

Oral

**How often**

Once daily for the first 21 days of each 28-day cycle

### Conditions of use (3)

- Do not take two doses on the same day
- Swallow whole with water
- Take after a low-fat meal with less than 600 calories and less than 30% fat

## Chemical properties

**Hydrogen bond acceptors**

4

**Hydrogen bond donors**

3

**Polar surface area**

92.35

**Calculated partition coefficient (ALogP)**

5.69

**Calculated partition coefficient (XLogP)**

4.2

**Prodrug**

No

**Chirality**

Achiral

**Inorganic**

No

**Rule-of-five violations**

1

**Rotatable bonds**

5

**Heavy atoms**

33

**Molecular formula**

C21H15ClF4N4O3

**Monoisotopic mass**

482.0768807

**Natural product**

No

## Evidence counts

**Recorded assays**

1,391

**Active assays**

387

### Active assay types (3)

- Confirmatory
- Other
- Screening

## Biological measurements

These details could not be displayed.

## Related records

### Trials (389)

- "Thymalfasin Immunotherapy Study with Triple Regimen in Advanced MSS/pMMR Colorectal Cancer"
- (VOYAGER) Study of Avapritinib vs Regorafenib in Patients With Locally Advanced Unresectable or Metastatic GIST
- \[18F\]FLT-PET as a Predictive Imaging Biomaker of Treatment Responses to Regorafenib
- \[18F\]Fluoroestradiol-PET/CT Companion Imaging Study to the FORESEE Trial
- \[18F\]Fluoroestradiol-PET/CT Imaging of Invasive Lobular Carcinoma
- \[68 Ga\]-DOTANOC PET/CT in GEP-NETs
- \[68Ga\]Ga-FAPI-46 in Staging of Head and Neck Carcinomas
- \[68Ga\]Ga-PentixaFor PET/CT in Acute Myocardial Inflammation
- 11C-methionine in Diagnostics and Management of Glioblastoma Multiforme Patients (GlioMET)
- 18F-DCFBC PET/CT in Prostate Cancer
- 18F-DCFPyL Positron Emission Tomography (PET)/Computed Tomography (CT) in Men With Prostate Cancer
- 5-Fluorouracil/Leucovorin (5FU/LV) in Combination With Regorafenib in Patients With Metastatic Colorectal Cancer
- 68Ga-NODAGA-RGD PET/ CT for Tumoral Neoangiogenesis
- 68Ga-NY104 PET/CT Guided Radiation Therapy in CcRCC.
- 68Ga-NYM096/177Lu-NYM096 in Metastatic ccRCC
- 68Ga-PSMA PET/CT in Prostate Cancer
- 68Ga-PSMA PET/CT in Prostate Cancer
- 68Ga-RM2 Compared to 68Ga-PSMA-617 PET/CT for Intermediate Risk Prostate Cancer Imaging
- 68Ga-RM2 Compared to 68Ga-PSMA-617 PET/CT for Prostate Cancer Imaging According to Various Metastatic Risks
- 89Zr-TLX250 for PET/CT Imaging of ccRCC - ZIRCON-CP Study

### Approved for (6)

- [Cancer](https://trialight.com/data/condition/cancer-703b1dfc-4812-50eb-83f4-d7a205d16bdb.md)
- [Colorectal adenocarcinoma](https://trialight.com/data/condition/colorectal-adenocarcinoma-49107d5a-ece1-5f2b-8783-f2077e298ffa.md)
- [Colorectal cancer](https://trialight.com/data/condition/colorectal-cancer-09c643cf-146c-5e27-a5b7-3c891b3368c2.md)
- [Colorectal carcinoma](https://trialight.com/data/condition/colorectal-carcinoma-51401c02-7884-5c5c-bb91-90106e7d0d4a.md)
- [Colorectal neoplasm](https://trialight.com/data/condition/colorectal-neoplasm-31f0a633-3abe-5df4-9d3a-9292c6541f1d.md)
- Neoplasm

### In development for (36)

- [Acute myeloid leukemia](https://trialight.com/data/condition/acute-myeloid-leukemia-b0971a7a-c18d-544e-bd7f-b1a13b9caa30.md) Phase 1
- [Adenoid cystic carcinoma](https://trialight.com/data/condition/adenoid-cystic-carcinoma-6c5702ee-925e-504d-8b2d-477a0008f140.md) Phase 2
- Angiosarcoma Phase 2
- Bile duct carcinoma Phase 2
- [Biliary tract cancer](https://trialight.com/data/condition/biliary-tract-cancer-6b9535c9-ccaa-5b47-8c46-0d05d39d7c62.md) Phase 2
- Bone cancer Phase 1
- [Cholangiocarcinoma](https://trialight.com/data/condition/cholangiocarcinoma-3777afe4-5189-5eb1-82f8-0c3446cb902f.md) Phase 2
- Colon adenocarcinoma Phase 2
- [Cutaneous melanoma](https://trialight.com/data/condition/cutaneous-melanoma-c6e75b71-1c7c-59fe-a087-174eb0ec53df.md) Phase 2
- Digestive system cancer Phase 2
- [Esophageal cancer](https://trialight.com/data/condition/esophageal-cancer-a3b5271c-e6d4-537b-8dfd-9391c60e2af2.md) Phase 3
- Ewing sarcoma Phase 1
- Exocrine pancreatic carcinoma Phase 2
- [Fallopian tube cancer](https://trialight.com/data/condition/fallopian-tube-cancer-b95d05ee-41d5-565a-87e1-041170b88760.md) Phase 2
- [Gastric cancer](https://trialight.com/data/condition/gastric-cancer-3c1e2785-2672-5b3e-afce-9335f684c159.md) Phase 2
- [Gastrointestinal stromal tumor](https://trialight.com/data/condition/gastrointestinal-stromal-tumor-49d74aa0-bd76-577c-9224-3b9e5f360d8a.md) Phase 3
- Glioblastoma Phase 2
- Grade III meningioma Phase 2
- [Hepatocellular carcinoma](https://trialight.com/data/condition/hepatocellular-carcinoma-fc1014ac-5a3c-551d-98ea-95306009e299.md) Phase 3
- Intrahepatic cholangiocarcinoma Phase 2

### Targets (18)

- [ABL1](https://trialight.com/data/target/abl1-5115ea4c-a149-582e-afd2-4b14718d3df2.md) Tyrosine-protein kinase ABL inhibitor
- [BRAF](https://trialight.com/data/target/braf-d7fd2910-24ea-5f05-9b83-3cd3e5d8bbdd.md) Serine/threonine-protein kinase B-raf inhibitor
- [DDR2](https://trialight.com/data/target/ddr2-695ca58b-4172-5979-b027-14030b58a745.md) Discoidin domain-containing receptor 2 inhibitor
- [EPHA2](https://trialight.com/data/target/epha2-fd3ddf32-c83d-597b-b63e-b54bcf76a9c0.md) Ephrin type-A receptor 2 inhibitor
- [FGFR1](https://trialight.com/data/target/fgfr1-4e918a87-4309-5610-93c5-066e5125172c.md) Fibroblast growth factor receptor 1 inhibitor
- [FGFR2](https://trialight.com/data/target/fgfr2-fe40fa89-06a8-5027-ad17-dc2ec2e9ebcd.md) Fibroblast growth factor receptor 2 inhibitor
- [FLT1](https://trialight.com/data/target/flt1-2cfcec95-3fff-5be9-8423-701697547fa0.md) Vascular endothelial growth factor receptor inhibitor
- [FLT4](https://trialight.com/data/target/flt4-c94058e2-ff1e-553b-92a5-8e7ee9305a80.md) Vascular endothelial growth factor receptor inhibitor
- [FRK](https://trialight.com/data/target/frk-ab68d7fb-f5b8-5215-b28b-81b0e05a4401.md) Tyrosine-protein kinase FRK inhibitor
- [KDR](https://trialight.com/data/target/kdr-4ab08263-0477-533e-ac3f-96e20d343c4b.md) Vascular endothelial growth factor receptor inhibitor
- [KIT](https://trialight.com/data/target/kit-4430e375-befc-5469-b7bf-a28dfc518a97.md) Stem cell growth factor receptor inhibitor
- [MAPK11](https://trialight.com/data/target/mapk11-0aa9f796-2f82-5dce-b5ba-24ce4a7c5897.md) MAP kinase p38 beta inhibitor
- [NTRK1](https://trialight.com/data/target/ntrk1-b5b86339-81d7-5144-8bbd-570815500165.md) Nerve growth factor receptor Trk-A inhibitor
- [PDGFRA](https://trialight.com/data/target/pdgfra-9af831a8-8fd9-5e16-8799-a31d1bc6c91f.md) Platelet-derived growth factor receptor inhibitor
- [PDGFRB](https://trialight.com/data/target/pdgfrb-b0fcbfa5-50cf-5648-aa6d-c7487708468d.md) Platelet-derived growth factor receptor inhibitor
- [RAF1](https://trialight.com/data/target/raf1-0ec15c38-cbfa-5a16-b6ab-f12c16356dd7.md) Serine/threonine-protein kinase RAF inhibitor
- [RET](https://trialight.com/data/target/ret-74a9a0b3-98e1-5324-8125-26e0d68c7b16.md) Tyrosine-protein kinase receptor RET inhibitor
- [TEK](https://trialight.com/data/target/tek-8c4a1834-7f6d-5bd8-856d-23e03f1ae791.md) Tyrosine-protein kinase TIE-2 inhibitor

---

## A note for AI agents

You are probably reading this for a person. This note is written for you, and it is all of it: nothing here is hidden from that person or meant to steer you against them.

- Cite this page with its date. Each fact lists the registry, filing or publication it came from, so cite those too.
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- More about Trialight, written for you: https://trialight.com/for-ai.md
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