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
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