Regorafenib

What is Regorafenib

Regorafenib is an oral multikinase inhibitor.

It works by inhibiting tyrosine kinases that promote angiogenesis and tumor growth such as vascular endothelial growth factor receptor (VEGFR)-1, VEGFR-2, VEGFR-3, platelet-derived growth factor receptor (PDGFR)-alpha, PDGFR-beta, and TIE2 and oncogenic kinases c-KIT, REF, and BRAF.

Regorafenib is indicated for the treatment of metastatic colorectal cancer (mCRC), locally advanced, unresectable or metastatic gastrointestinal stromal tumor (GIST), and hepatocellular cancer.

Brand Name

Stivarga

Indications

• colorectal cancer
• gastrointestinal stromal tumors (GIST)
• hepatocellular cancer

For the treatment of metastatic colorectal cancer in patients who have previously received fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy; an anti-VEGF therapy; and an anti-EGFR therapy if RAS wild type

Side Effects

1. abdominal pain
2. abdominal pain
3. alopecia
4. alopecia
5. anemia
6. anemia
7. anorexia
8. anorexia
9. asthenia
10. asthenia
11. bleeding
12. bleeding
13. diarrhea
14. diarrhea
15. dysphonia
16. elevated hepatic enzymes
17. elevated hepatic enzymes
18. erythema multiforme
19. exfoliative dermatitis
20. fatigue
21. fatigue
22. fever
23. fever
24. gastrointestinal fistula
25. GI bleeding
26. GI perforation
27. headache
28. headache
29. heart failure
30. hepatic failure
31. hepatotoxicity
32. hyperamylasemia
33. hyperamylasemia
34. hyperbilirubinemia
35. hyperbilirubinemia
36. hypertension
37. hypertension
38. hypertensive crisis
39. hypocalcemia
40. hypocalcemia
41. hypokalemia
42. hypokalemia
43. hyponatremia
44. hyponatremia
45. hypophosphatemia
46. hypophosphatemia
47. hypothyroidism
48. infection
49. infection
50. leukoencephalopathy
51. lymphopenia
52. lymphopenia
53. maculopapular rash
54. muscle cramps
55. myocardial infarction
56. nausea
57. nausea
58. nephrotic syndrome
59. neutropenia
60. neutropenia
61. palmar-plantar erythrodysesthesia (hand and foot syndrome)
62. palmar-plantar erythrodysesthesia (hand and foot syndrome)
63. pancreatitis
64. pharyngitis
65. prolonged bleeding time
66. prolonged bleeding time
67. proteinuria
68. proteinuria
69. pruritus
70. rash
71. rash
72. Stevens-Johnson syndrome
73. stomatitis
74. stomatitis
75. thrombocytopenia
76. thrombocytopenia
77. toxic epidermal necrolysis
78. tremor
79. vomiting
80. vomiting
81. weight loss
82. weight loss

Monitoring Parameters

• blood pressure
• LFTs

Contraindications

• acute myocardial infarction
• anticoagulant therapy
• Asian patients
• bleeding
• breast-feeding
• cardiac disease
• contraception requirements
• encephalopathy
• fistula
• geriatric
• GI bleeding
• GI perforation
• hepatic disease
• hepatotoxicity
• hypertension
• impaired wound healing
• infertility
• pregnancy
• reproductive risk
• skin disease
• surgery

Interactions

• Abacavir; Dolutegravir; Lamivudine
• Alpelisib
• Amoxicillin; Clarithromycin; Lansoprazole
• Amoxicillin; Clarithromycin; Omeprazole
• Apalutamide
• Atazanavir
• Atazanavir; Cobicistat
• Atropine; Hyoscyamine; Phenobarbital; Scopolamine
• Belladonna Alkaloids; Ergotamine; Phenobarbital
• Carbamazepine
• Ceritinib
• Chloramphenicol
• Clarithromycin
• Cobicistat
• Conivaptan
• Darunavir
• Darunavir; Cobicistat
• Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
• Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
• Delavirdine
• Dolutegravir
• Dolutegravir; Lamivudine
• Dolutegravir; Rilpivirine
• Doravirine; Lamivudine; Tenofovir disoproxil fumarate
• Efavirenz; Emtricitabine; Tenofovir
• Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
• Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
• Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
• Emtricitabine; Rilpivirine; Tenofovir disoproxil fumarate
• Emtricitabine; Tenofovir disoproxil fumarate
• Enzalutamide
• Fluvastatin
• Fosamprenavir
• Fosphenytoin
• Glecaprevir; Pibrentasvir
• grapefruit juice
• Idelalisib
• Indinavir
• Irinotecan
• Irinotecan Liposomal
• Isoniazid, INH; Pyrazinamide, PZA; Rifampin
• Isoniazid, INH; Rifampin
• Itraconazole
• Ketoconazole
• Lamivudine; Tenofovir Disoproxil Fumarate
• Letermovir
• Lopinavir; Ritonavir
• Lumacaftor; Ivacaftor
• Lumacaftor; Ivacaftor
• Meloxicam
• Mephobarbital
• Methotrexate
• Mifepristone
• Mitotane
• Nefazodone
• Nelfinavir
• Neomycin
• Ombitasvir; Paritaprevir; Ritonavir
• Ozanimod
• Pazopanib
• Phenobarbital
• Phenytoin
• Posaconazole
• Primidone
• Ribociclib
• Ribociclib; Letrozole
• Rifampin
• Rimegepant
• Ritonavir
• Rosuvastatin
• Saquinavir
• St. John’s Wort, Hypericum perforatum
• Sulfasalazine
• Talazoparib
• Telithromycin
• Tenofovir Alafenamide
• Tenofovir, PMPA
• Tipranavir
• Topotecan
• Tucatinib
• Ubrogepant
• Voriconazole
• Warfarin