General Information of Drug (ID: DMHSY1I)

Drug Name
Regorafenib Drug Info
Synonyms
Regorafenib; 755037-03-7; BAY 73-4506; Regorafenibum; Stivarga; 4-(4-(3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide; BAY73-4506; Regorafenib (BAY 73-4506); UNII-24T2A1DOYB; 4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide; BAY-73-4506; 24T2A1DOYB; CHEMBL1946170; CHEBI:68647; Stivarga (TN); BAY73-4506 hydrochloride; Regorafenib [USAN:INN]
Indication
Disease Entry ICD 11 Status REF
Gastrointestinal stromal tumour 2B5B Approved [1]
Metastasis from malignant tumor of colon Approved [1]
Metastatic colorectal cancer 2B91 Approved [2]
Cross-matching ID
PubChem CID
11167602
ChEBI ID
CHEBI:68647
CAS Number
CAS 755037-03-7
TTD Drug ID
DMHSY1I
VARIDT Drug ID
DR00136
INTEDE Drug ID
DR1401
ACDINA Drug ID
D00586

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [10]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [11]
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [12]
Ponatinib DMYGJQO Acute lymphoblastic leukaemia 2A85 Approved [3]
Pazopanib HCl DM6U9CQ Renal cell carcinoma 2C90 Approved [13]
Pexidartinib DMS2J0Z Tenosynovial giant cell tumour 2F7B Approved [14]
Ripretinib DM958QB Gastrointestinal stromal tumour 2B5B Approved [15]
Famitinib DMSFWT7 Solid tumour/cancer 2A00-2F9Z Phase 2 [16]
XL-820 DMMHX9K Solid tumour/cancer 2A00-2F9Z Phase 2 [17]
MP470 DMELUAK Solid tumour/cancer 2A00-2F9Z Phase 2 [18]
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Drug(s) Targeting Proto-oncogene c-Ret (RET)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [19]
Ponatinib DMYGJQO Acute lymphoblastic leukaemia 2A85 Approved [3]
Vandetanib DMRICNP Solid tumour/cancer 2A00-2F9Z Approved [10]
Selpercatinib DMZR15V Non-small-cell lung cancer 2C25.Y Approved [20]
Pralsetinib DMWU0I2 Non-small-cell lung cancer 2C25.Y Approved [21]
MGCD516 DM752PU Solid tumour/cancer 2A00-2F9Z Phase 2/3 [22]
CEP-32496 DMAO04B Solid tumour/cancer 2A00-2F9Z Phase 1/2 [23]
TPX-0046 DMIVE67 Solid tumour/cancer 2A00-2F9Z Phase 1/2 [24]
GSK3179106 DM2KCIP Inflammatory bowel disease DD72 Phase 1 [25]
BOS172738 DM9L0D8 Solid tumour/cancer 2A00-2F9Z Phase 1 [26]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [11]
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [27]
Sunitinib DMCBJSR Acute undifferentiated leukemia Approved [28]
Axitinib DMGVH6N Renal cell carcinoma 2C90 Approved [29]
Vandetanib DMRICNP Solid tumour/cancer 2A00-2F9Z Approved [10]
Pazopanib HCl DM6U9CQ Renal cell carcinoma 2C90 Approved [13]
Fruquintinib DMHOSCQ Colorectal cancer 2B91.Z Approved [30]
Cabozantinib DMIYDT4 Medullary thyroid gland carcinoma Approved [31]
Tivozanib DMUKC5L Renal cell carcinoma 2C90 Approved [32]
Lenvatinib DMB1IU4 Thyroid cancer 2D10 Approved [33]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [34]
Methotrexate DM2TEOL Anterior urethra cancer Approved [35]
Folic Acid DMEMBJC Colorectal carcinoma Approved [36]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [37]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [38]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [39]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [40]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [41]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [42]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [43]
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Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [44]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [45]
Methotrexate DM2TEOL Anterior urethra cancer Approved [46]
Folic Acid DMEMBJC Colorectal carcinoma Approved [47]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [46]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [46]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [48]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [46]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [49]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [50]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [51]
Methotrexate DM2TEOL Anterior urethra cancer Approved [52]
Folic Acid DMEMBJC Colorectal carcinoma Approved [53]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [54]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [55]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [56]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [57]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [56]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [58]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [59]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [60]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [61]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [62]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [63]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [62]
Pravastatin DM6A0X7 Adult acute monocytic leukemia Approved [64]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [65]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [66]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [67]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [64]
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Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [68]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [69]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [70]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [71]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [72]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [73]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [74]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [75]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [69]
Verapamil DMA7PEW Angina pectoris BA40 Approved [76]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [77]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [78]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [79]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [76]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [80]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [76]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [76]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [81]
Nateglinide DMLK2QH Diabetic complication 5A2Y Approved [76]
Haloperidol DM96SE0 Delirium Approved [76]
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Drug(s) Affected By Poly polymerase 1 (PARP1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [82]
Gefitinib DM15F0X Colon adenocarcinoma Approved [83]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [84]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [85]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [86]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [87]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [86]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [88]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [89]
Methotrexate DM2TEOL Anterior urethra cancer Approved [90]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [91]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [92]
Gefitinib DM15F0X Colon adenocarcinoma Approved [93]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [94]
Selenium DM25CGV N. A. N. A. Approved [95]
Pentosan Polysulfate DM2HRKE Interstitial cystitis GC00.3 Approved [96]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [88]
Methotrexate DM2TEOL Anterior urethra cancer Approved [97]
Dactinomycin DM2YGNW Adult kidney Wilms tumor Approved [98]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [99]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Halothane DM80OZ5 Anaesthesia 9A78.6 Approved [100]
Isoniazid DM5JVS3 Latent tuberculosis infection Approved [101]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [102]
Primidone DM0WX6I Epilepsy 8A60-8A68 Approved [100]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [100]
Cocaine DMSOX7I Anaesthesia 9A78.6 Approved [100]
Gefitinib DM15F0X Colon adenocarcinoma Approved [8]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [103]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [8]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [8]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Indomethacin DMSC4A7 Bursitis Approved [104]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [105]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [106]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [107]
Gefitinib DM15F0X Colon adenocarcinoma Approved [108]
Talazoparib DM1KS78 Breast cancer 2C60-2C65 Approved [109]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [110]
Selenium DM25CGV N. A. N. A. Approved [111]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [112]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [113]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [114]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [115]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [85]
Methotrexate DM2TEOL Anterior urethra cancer Approved [116]
Epinephrine DM3KJBC Acute asthma CA23 Approved [117]
Quercetin DM3NC4M Obesity 5B81 Approved [118]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [119]
Fructose DM43AN2 Vomiting MD90 Approved [120]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [114]
Cyclophosphamide DM4O2Z7 Advanced cancer 2A00-2F9Z Approved [121]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [122]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [123]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [124]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [125]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [126]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [127]
Secobarbital DM14RF5 Epilepsy 8A60-8A68 Approved [128]
Gefitinib DM15F0X Colon adenocarcinoma Approved [129]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [130]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [131]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Ethanol DMDRQZU Chronic pain MG30 Approved [132]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [123]
Carvedilol DMHTEAO Chronic heart failure BD1Z Approved [133]
Paclitaxel DMLB81S Breast carcinoma Approved [134]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [135]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [122]
Urokinase DM0GOUD Myocardial infarction BA41-BA43 Approved [100]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [136]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [125]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [126]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Caspase-3 (CASP3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sevoflurane DMC9O43 Anaesthesia 9A78.6 Approved [137]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [138]
Lovastatin DM9OZWQ Arteriosclerosis BD40 Approved [139]
Cidofovir DMA13GD Cytomegalovirus infection 1D82 Approved [140]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [141]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [142]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [143]
Mannitol DMSCDY9 Bronchiectasis CA24 Approved [144]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [145]
Aprepitant DM053KT Depression 6A70-6A7Z Approved [146]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [147]
Gefitinib DM15F0X Colon adenocarcinoma Approved [148]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [149]
Epinephrine DM3KJBC Acute asthma CA23 Approved [117]
Quercetin DM3NC4M Obesity 5B81 Approved [150]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [151]
Fructose DM43AN2 Vomiting MD90 Approved [120]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [152]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [153]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [154]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [136]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [106]
Selenium DM25CGV N. A. N. A. Approved [111]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [155]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [156]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [157]
Quercetin DM3NC4M Obesity 5B81 Approved [158]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [159]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [160]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [161]
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Drug(s) Affected By Caspase-8 (CASP8)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Lovastatin DM9OZWQ Arteriosclerosis BD40 Approved [162]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [163]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [164]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [136]
Gefitinib DM15F0X Colon adenocarcinoma Approved [148]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [165]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [85]
Selenium DM25CGV N. A. N. A. Approved [111]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [166]
Methotrexate DM2TEOL Anterior urethra cancer Approved [167]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Proto-oncogene c-Ret (RET) TT4DXQT RET_HUMAN Modulator [3]
Tyrosine-protein kinase Kit (KIT) TTX41N9 KIT_HUMAN Modulator [3]
Vascular endothelial growth factor receptor 2 (KDR) TTUTJGQ VGFR2_HUMAN Modulator [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Substrate [4]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [5]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [4]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [6]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [7]
UDP-glucuronosyltransferase 1A9 (UGT1A9) Main DME DE85D2P UD19_HUMAN Substrate [7]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Alanine aminotransferase 1 (GPT) OTOXOA0Q ALAT1_HUMAN Protein Interaction/Cellular Processes [8]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Gene/Protein Processing [9]
Caspase-8 (CASP8) OTA8TVI8 CASP8_HUMAN Gene/Protein Processing [9]
E3 ubiquitin-protein ligase XIAP OT24GP9B XIAP_HUMAN Gene/Protein Processing [9]
G1/S-specific cyclin-D1 (CCND1) OT8HPTKJ CCND1_HUMAN Gene/Protein Processing [9]
Matrix metalloproteinase-9 (MMP9) OTB2QDAV MMP9_HUMAN Gene/Protein Processing [9]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Post-Translational Modifications [9]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Post-Translational Modifications [9]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Protein Interaction/Cellular Processes [9]
Transcription factor p65 (RELA) OTUJP9CN TF65_HUMAN Gene/Protein Processing [9]

References

1 Regorafenib FDA Label
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5891).
3 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
4 Regorafenib is transported by the organic anion transporter 1B1 and the multidrug resistance protein 2. Biol Pharm Bull. 2015;38(4):582-6.
5 KEGG: new perspectives on genomes, pathways, diseases and drugs. Nucleic Acids Res. 2017 Jan 4;45(D1):D353-D361. (dg:DG01913)
6 Brain and Testis Accumulation of Regorafenib is Restricted by Breast Cancer Resistance Protein (BCRP/ABCG2) and P-glycoprotein (P-GP/ABCB1). Pharm Res. 2015 Jul;32(7):2205-16.
7 FDA Label of Regorafenib. The 2020 official website of the U.S. Food and Drug Administration.
8 Cytotoxicity of 34 FDA approved small-molecule kinase inhibitors in primary rat and human hepatocytes. Toxicol Lett. 2018 Jul;291:138-148. doi: 10.1016/j.toxlet.2018.04.010. Epub 2018 Apr 12.
9 Regorefenib induces extrinsic/intrinsic apoptosis and inhibits MAPK/NF-B-modulated tumor progression in bladder cancer in vitro and in vivo. Environ Toxicol. 2019 Jun;34(6):679-688. doi: 10.1002/tox.22734. Epub 2019 Feb 25.
10 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
11 Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling.Mol Cancer Ther.2008 Oct;7(10):3129-40.
12 New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven a... J Med Chem. 2000 Jun 15;43(12):2310-23.
13 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
14 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
15 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
16 Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
17 National Cancer Institute Drug Dictionary (drug id 452042).
18 Phase 1B study of amuvatinib in combination with five standard cancer therapies in adults with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Jul;74(1):195-204.
19 Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. Bioorg Med Chem. 2010 Feb 15;18(4):1482-96.
20 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
21 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
22 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2185).
23 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
24 Clinical pipeline report, company report or official report of Turning Point Therapeutics.
25 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
26 National Cancer Institute Drug Dictionary (drug name Zeteletinib).
27 Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
28 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
29 Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
30 Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45.
31 Clinical pipeline report, company report or official report of Exelixis (2011).
32 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services
33 Emerging drugs for ovarian cancer. Expert Opin Emerg Drugs. 2008 Sep;13(3):523-36.
34 Involvement of the drug transporters p glycoprotein and multidrug resistance-associated protein Mrp2 in telithromycin transport. Antimicrob Agents Chemother. 2006 Jan;50(1):80-7.
35 Dose-dependent disposition of methotrexate in Abcc2 and Abcc3 gene knockout murine models. Drug Metab Dispos. 2011 Nov;39(11):2155-61.
36 Mammalian multidrug-resistance proteins (MRPs). Essays Biochem. 2011 Sep 7;50(1):179-207.
37 Enhancing chemosensitivity in oral squamous cell carcinoma by lentivirus vector-mediated RNA interference targeting EGFR and MRP2. Oncol Lett. 2016 Sep;12(3):2107-2114.
38 Multidrug resistance associated protein 2 mediates transport of prostaglandin E2. Liver Int. 2006 Apr;26(3):362-8.
39 Lentivirus-mediated RNAi silencing targeting ABCC2 increasing the sensitivity of a human nasopharyngeal carcinoma cell line against cisplatin. J Transl Med. 2008 Oct 4;6:55.
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