Stivarga 40mg | Regorafenib 40mg
Apple Pharmaceuticals
Stivarga 40mg tablets (Regorafenib)
Stivarga is an antineoplastic drug which prohibit with the growth and spread of cancer cells in the body.
Stivarga 40mg is needed to treat colorectal cancer and liver cancer. It is also needed to treat a rare type of tumor which can affect the oesophagus, stomach, or intestines.
Stivarga 40mg tablets is commonly given after other cancer regimens have been tried without success.
Stivarga 40mg is needed to treat colorectal cancer and liver cancer. It is also needed to treat a rare type of tumor which can affect the oesophagus, stomach, or intestines.
Stivarga 40mg tablets is commonly given after other cancer regimens have been tried without success.
INDICATION
Stivarga 40mg is indicated for the treatment of metastatic colorectal cancer (CRC) who have been previously treated with, or are not considered candidates for, available therapies. These contains fluoropyrimidine-based chemotherapy, an anti-VEGF therapy and an anti-EGFR therapy (see section 5.1)
Stivarga 40mg is indicated for the treatment of unresectable or metastatic gastrointestinal stromal tumours (GIST) who progressed on or are intolerant to prior treatment with imatinib and sunitinib
Stivarga 40mg tablet is indicated for the treatment of hepatocellular carcinoma (HCC) who have been previously treated with sorafenib.
Stivarga 40mg is indicated for the treatment of unresectable or metastatic gastrointestinal stromal tumours (GIST) who progressed on or are intolerant to prior treatment with imatinib and sunitinib
Stivarga 40mg tablet is indicated for the treatment of hepatocellular carcinoma (HCC) who have been previously treated with sorafenib.
DOSAGE
Colorectal cancer :
The usual dose is 160mg (four 40mg tablets) Po q Day for the first 21 days of each 28-day cycle.
Gastrointestinal stromal tumor :
The usual dose is 160mg (four 40mg tablets) Po q Day for the first 21 days of each 28-day cycle.
Hepatocellular carcinoma :
The usual dose is 160mg (four 40mg tablets) Po q Day for the first 21 days of each 28-day cycle.
Follow the treatment of this conditions until disease progression or undesirable toxicity
The usual dose is 160mg (four 40mg tablets) Po q Day for the first 21 days of each 28-day cycle.
Gastrointestinal stromal tumor :
The usual dose is 160mg (four 40mg tablets) Po q Day for the first 21 days of each 28-day cycle.
Hepatocellular carcinoma :
The usual dose is 160mg (four 40mg tablets) Po q Day for the first 21 days of each 28-day cycle.
Follow the treatment of this conditions until disease progression or undesirable toxicity
MECHANISM
Regorafenib belongs to oral tumour deactivation agent which potently stops multiple protein kinases, contain kinases included in tumour angiogenesis (VEGFR1, -2, -3, TIE2), oncogenesis (KIT, RET, RAF-1, BRAF, BRAFV600E), metastasis (VEGFR3, PDGFR, FGFR) and tumour immunity (CSF1R). Regorafenib prohibits mutated KIT, a major oncogenic driver in gastrointestinal stromal tumours, and thereby stops tumour cell multiplication. In preclinical studies regorafenib has described potent anticancer activity in a broad spectrum of tumour models containing colorectal, gastrointestinal stromal and hepatocellular tumour models which is likely mediated by its anti-angiogenic and anti-proliferative effects. In addition, regorafenib decreased the levels of tumour analogue macrophages and has shown anti-metastatic effects in vivo. Major human metabolites (M-2 and M-5) displayed similar efficacies, compared to regorafenib in in vitro and in vivo models.
ADME
Absorption:
time to peak plasma is 4 hours and concentration is 2.5mcg/mL for single dose; 3.9mcg/mL for steady state and bioavailability is 69-83%
Distribution:
regorafenib has protein bounding about 99.5% and M-2 active metabolite is 99.8%; M-5 active metabolite is 99.95%
Metabolism:
Regorafenib is metabolized by CYP3A4 and UGT1A9
Elimination:
excreted via feces 71%; 19% urine (within 12 days of single dose)
Half-life of
Regorafenib is 28 hr
M-2 active metabolite is 25 hr
M-5 active metabolite is 51hr
time to peak plasma is 4 hours and concentration is 2.5mcg/mL for single dose; 3.9mcg/mL for steady state and bioavailability is 69-83%
Distribution:
regorafenib has protein bounding about 99.5% and M-2 active metabolite is 99.8%; M-5 active metabolite is 99.95%
Metabolism:
Regorafenib is metabolized by CYP3A4 and UGT1A9
Elimination:
excreted via feces 71%; 19% urine (within 12 days of single dose)
Half-life of
Regorafenib is 28 hr
M-2 active metabolite is 25 hr
M-5 active metabolite is 51hr
PRECAUTION
Myocardial ischemia and infarction seen in clinical trials; withhold Stivarga for new or acute cardiac ischemia/infarction and restart only after resolution of acute ischemic events
While treatment with Stivarga, one case report of reversible posterior leukoencephalopathy syndrome (RPLS) reported (1 of 1100 treated patients); interrupt therapy if RPLS occurs
serious drug-induced liver injury with fatal outcome appeared in Stivarga-treated patients in clinical trials. Some of the cases, liver dysfunction resulted within the first 2 months of treatment and was characterized by a hepatocellular pattern of injury.
While treatment with Stivarga 40mg will Increases risk for haemorrhage; stop therapy for severe or life-threatening haemorrhage
While treatment with Stivarga will Increased risk of infections resulted; most common infections contains urinary tract infections, nasopharyngitis, mucocutaneous and systemic fungal infections and pneumonia
While treatment with Stivarga will Increases risk for HFSR/PPES and rash; a higher incidence of HFSR resulted in Asian patients; discontinue and then decrease or stop regorafenib depending on severity and persistence of dermatologic toxicity
While treatment with Stivarga, one case report of reversible posterior leukoencephalopathy syndrome (RPLS) reported (1 of 1100 treated patients); interrupt therapy if RPLS occurs
serious drug-induced liver injury with fatal outcome appeared in Stivarga-treated patients in clinical trials. Some of the cases, liver dysfunction resulted within the first 2 months of treatment and was characterized by a hepatocellular pattern of injury.
While treatment with Stivarga 40mg will Increases risk for haemorrhage; stop therapy for severe or life-threatening haemorrhage
While treatment with Stivarga will Increased risk of infections resulted; most common infections contains urinary tract infections, nasopharyngitis, mucocutaneous and systemic fungal infections and pneumonia
While treatment with Stivarga will Increases risk for HFSR/PPES and rash; a higher incidence of HFSR resulted in Asian patients; discontinue and then decrease or stop regorafenib depending on severity and persistence of dermatologic toxicity
DRUG INTERACTION
Stivarga concomitant use with strong CYP3A4 inducers will decrease Regorafenib plasma concentrations and increased plasma concentration of active metabolite M-2; M-5.
Stivarga 40mg interaction with strong CYP3A4 inhibitor will increase Regorafenib plasma concentration and reduced plasma concentration of active metabolite M-2; M-5.
Stivarga 40mg Tablets interaction with BCRP substrate will increased the plasma concentration of the BCRP substrate.
Stivarga 40mg interaction with strong CYP3A4 inhibitor will increase Regorafenib plasma concentration and reduced plasma concentration of active metabolite M-2; M-5.
Stivarga 40mg Tablets interaction with BCRP substrate will increased the plasma concentration of the BCRP substrate.
MISSED DOSE
If dose is missed, patients must consult with medical practitioner and follow the instructions given by them. Thereby missed dose should be avoid and follow the regular dosing schedule
STORAGE
Store the Stivarga 40mg at 25℃ (77℃)
Keep the drug in its original container bottle
Keep the bottle tightly closed after one time used
Keep the drug in its original container bottle
Keep the bottle tightly closed after one time used
SIDE EFFECTS
Common side effects occurring in greater than 30% :
Hand-foot syndrome , Diarrhea, Low platelets, Mouth sores/inflammation, Weight loss, Infection, Anemia, Increased liver enzymes (AST, ALT), Fatigue, High blood pressure, Voice disorder (Dysphonia), Protein in the urine, Low calcium, Low phosphorous, Low white blood cells, Decreased appetite, Increased lipase & amylase, High bilirubin in the blood, Low sodium, Nausea.
Less common side effects occurring in about 10-29% of patients receiving Stivarga 40mg :
Pain, Fever, Rash, Low potassium, Decreased blood clotting, Increased bleeding, Headache, Alopecia.
Hand-foot syndrome , Diarrhea, Low platelets, Mouth sores/inflammation, Weight loss, Infection, Anemia, Increased liver enzymes (AST, ALT), Fatigue, High blood pressure, Voice disorder (Dysphonia), Protein in the urine, Low calcium, Low phosphorous, Low white blood cells, Decreased appetite, Increased lipase & amylase, High bilirubin in the blood, Low sodium, Nausea.
Less common side effects occurring in about 10-29% of patients receiving Stivarga 40mg :
Pain, Fever, Rash, Low potassium, Decreased blood clotting, Increased bleeding, Headache, Alopecia.
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