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These brands contain the same active ingredient (Regorafenib Monohydrate). Same strength and form. Confirm the switch with your doctor or pharmacist.
Indications & Uses
Regorafenib Monohydrate is used to treat metastatic colorectal cancer (CRC) in patients who have already been treated with fluoropyrimidine, oxaliplatin and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if the cancer is RAS wild-type, an anti-EGFR therapy. The same use is stated again for colorectal cancer: the medicine is indicated for patients with metastatic colorectal cancer (CRC) whose earlier treatment included fluoropyrimidine, oxaliplatin and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if RAS wild-type, an anti-EGFR therapy. For gastrointestinal stromal tumors, Regorafenib Monohydrate is indicated in patients with locally advanced, unresectable or metastatic gastrointestinal stromal tumor (GIST) who have been treated before with Imatinib Mesylate and Sunitinib Malate. It is also indicated for hepatocellular carcinoma (HCC) in patients who have previously been treated with Sorafenib.
Pharmacology
Regorafenib is a small molecule that blocks many kinases, both those in the cell membrane and those inside the cell. These kinases are involved in normal cell functions and also in disease processes such as oncogenesis, tumor angiogenesis, metastasis and tumor immunity. In vitro biochemical or cellular assays showed that regorafenib or its major human active metabolites M-2 and M-5 inhibited the activity of RET, VEGFR1, VEGFR2, VEGFR3, KIT, PDGFR-alpha, PDGFR-beta, FGFR1, FGFR2, TIE2, DDR2, TrkA, Eph2A, RAF-1, BRAF, BRAF V600E, SAPK2, PTK5, Abl and CSF1R. This happened at concentrations that have been reached in patients. In vivo, the drug showed anti-angiogenic activity in a rat tumor model and inhibited tumor growth in several mouse xenograft models, including some for human colorectal carcinoma, gastrointestinal stromal and hepatocellular carcinoma. It also showed anti-metastatic activity in a mouse xenograft model and in two mouse orthotopic models of human colorectal carcinoma.
The effect of multiple doses (160 mg once daily for 21 days) on the QTc interval was studied in an open-label, single-arm study of 25 patients with advanced solid tumors. The study found no large changes in the mean QTc interval (that is, more than 20 msec).
Absorption: After a single 160 mg dose in patients with advanced solid tumors, the geometric mean peak plasma level (Cmax) is 2.5 µg/mL, reached at a median time of 4 hours. The geometric mean area under the plasma concentration vs. time curve (AUC) is 70.4 µg*h/mL. At steady-state, the AUC increases less than dose proportionally at doses greater than 60 mg. The geometric mean Cmax at steady-state is 3.9 µg/mL and the geometric mean AUC is 58.3 µg/h/mL. The coefficient of variation of AUC and Cmax is between 35% and 44%. Compared with an oral solution, the mean relative bioavailability of the tablets is 69% to 83%.
Distribution: The medicine undergoes enterohepatic circulation, so several plasma concentration peaks are seen across the 24-hour dosing interval. It is highly bound (99.5%) to human plasma proteins.
Elimination: After a single 160 mg oral dose, the geometric mean (minimum to maximum) elimination half-life in plasma is 28 hours (14 to 58 hours) for regorafenib and 25 hours (14 to 32 hours) for the M-2 metabolite. M-5 has a longer mean (minimum to maximum) elimination half-life of 51 hours (32 to 70 hours).
Metabolism: CYP3A4 and UGT1A9 metabolize the drug. The main metabolites circulating in human plasma at steady-state are M-2 (N-oxide) and M-5 (N-oxide and N-desmethyl). Both have in vitro pharmacological activity and steady-state concentrations similar to the parent drug. M-2 and M-5 are highly protein bound (99.8% and 99.95%, respectively).
Excretion: In a study using a radiolabeled oral solution at a dose of 120 mg, about 71% of the dose was excreted in feces within 12 days after administration (47% as parent compound, 24% as metabolites). About 19% of the dose was excreted in urine (17% as glucuronides) in the same period.
Dosage Reference
Reference Information Only
Dosages shown are general references from official sources. Always consult your doctor or pharmacist for personalized dosing.
Adults:
The recommended dose of Regorafenib is 160 mg (four 40 mg tablets) taken by mouth once daily for the first 21 days of each 28-day cycle. Treatment continues until the disease gets worse or the side effects become unacceptable. Take Regorafenib at the same time each day. Swallow each tablet whole with water, after a low-fat meal that contains less than 600 calories and less than 30% fat. If you miss a dose, don't take two doses of Regorafenib on the next day to make up for it.
Dose Modifications
If the dose needs to be changed, it is reduced in steps of 40 mg (one tablet). The lowest recommended daily dose of Regorafenib is 80 mg. Or, as directed by the registered physicians.
Pediatric Use
The safety and efficacy of Regorafenib in patients under 18 years of age have not been established.
Side Effects
Hepatotoxicity, infections, hemorrhage, gastrointestinal perforation or fistula, dermatological toxicity, hypertension, cardiac ischemia and infarction, Reversible Posterior Leukoencephalopathy Syndrome (RPLS).
Cautions & Contraindications
Warnings & Precautions
Hepatotoxicity: Severe drug-induced liver injury, some of it fatal, occurred in patients treated with Regorafenib Monohydrate in clinical trials. In most cases the liver problem appeared within the first 2 months of therapy and showed a hepatocellular pattern of injury. Liver function tests (ALT, AST and bilirubin) should be done before Regorafenib Monohydrate is started, then checked at least every two weeks during the first 2 months of treatment. Depending on how severe and how persistent the hepatotoxicity is, as shown by raised liver function tests or hepatocellular necrosis, the medicine should be held for a time and then either reduced in dose or stopped permanently. Infections: Regorafenib Monohydrate raised the risk of infections. The most common were urinary tract infections (5.7%), nasopharyngitis (4.0%), mucocutaneous and systemic fungal infections (3.3%) and pneumonia (2.6%). Deaths from infection were more frequent in patients on Regorafenib Monohydrate (1.0%) than in those given placebo (0.3%). The most common fatal infections were respiratory (0.6% in Regorafenib Monohydrate-treated patients vs 0.2% in patients receiving placebo). The medicine should be withheld for Grade 3 or 4 infections, or for an infection of any grade that is getting worse. It should be restarted at the same dose once the infection has resolved. Hemorrhage: Regorafenib Monohydrate caused more hemorrhage. Fatal hemorrhagic events occurred in 0.7% of patients, involving the central nervous system or the respiratory, gastrointestinal or genitourinary tracts. In patients with severe or life-threatening hemorrhage, Regorafenib Monohydrate should be stopped permanently. INR levels should be checked more often in patients who are taking Warfarin. Gastrointestinal Perforation or Fistula: Across all clinical trials where Regorafenib Monohydrate was given as a single agent, gastrointestinal perforation occurred in 0.6% of 4518 patients, and this included eight fatal events. Patients who develop gastrointestinal perforation or fistula should have Regorafenib Monohydrate stopped permanently. Dermatologic Toxicity: Hand-foot skin reaction (HFSR) was seen more often in Asian patients treated with Regorafenib Monohydrate (all grades: 72%, Grade 3: 18%). Depending on how severe and persistent the skin toxicity is, the medicine should be withheld, the dose reduced, or the treatment stopped permanently. Supportive measures should be started for symptomatic relief. Hypertension: Regorafenib Monohydrate increased the occurrence of hypertension (30% versus 8% in CORRECT, 59% versus 27% in GRID, and 31% versus 6% in RESORCE). In most patients who developed hypertension, it began during the first cycle of treatment (67% in randomized, placebo-controlled trials). Treatment should not be started unless blood pressure is well controlled. Blood pressure should be monitored weekly for the first 6 weeks and then every cycle, or more often if clinically indicated. For severe or uncontrolled hypertension, Regorafenib Monohydrate should be withheld, either temporarily or permanently. Cardiac Ischemia and Infarction: In randomized placebo-controlled trials, Regorafenib Monohydrate increased myocardial ischemia and infarction (0.9% vs 0.2%). It should be withheld in patients who develop new or acute onset cardiac ischemia or infarction. It should be resumed only after the acute cardiac ischemic events have resolved, and only if the potential benefits outweigh the risks of further cardiac ischemia. Reversible Posterior Leukoencephalopathy Syndrome (RPLS): RPLS is a syndrome of subcortical vasogenic edema, diagnosed by characteristic findings on MRI. It occurred in one of 1200 Regorafenib Monohydrate-treated patients across all clinical trials. Any patient who has seizures, severe headache, visual disturbances, confusion or altered mental function should be evaluated for RPLS. Regorafenib Monohydrate should be discontinued in patients who develop RPLS. Wound Healing Complications: No formal studies have been done on the effect of Regorafenib Monohydrate on wound healing. Vascular endothelial growth factor receptor (VEGFR) inhibitors such as Regorafenib Monohydrate can impair wound healing, so treatment should be discontinued at least 2 weeks before scheduled surgery. Whether to resume it after surgery should be decided by clinical judgment of adequate wound healing. Patients with wound dehiscence should have Regorafenib Monohydrate discontinued. Embryo-Fetal Toxicity: There are no data on the use of Regorafenib Monohydrate in pregnant women. Pregnant women should be told about the potential risk to a fetus. Females of reproductive potential should be advised to use effective contraception during treatment and for 2 months after the final dose. Males with female partners of reproductive potential should be advised the same, during treatment and for 2 months after the final dose.
Contraindications
Regorafenib Monohydrate must not be given to anyone who is known to be hypersensitive to Regorafenib or to any other component of the product.
Pregnancy & Breastfeeding
No data are available on the use of Regorafenib in pregnant women, but pregnant women should still be told about the possible hazard to the fetus. Nobody knows yet whether Regorafenib or its metabolites pass into human milk, what effect Regorafenib has on a breastfed infant, or whether it changes milk production. Because breastfed infants could have serious adverse reactions, a mother should not breastfeed during treatment with Regorafenib and for 2 weeks after the final dose.
Female reproductive potential: Effective contraception should be used during treatment and for 2 months after therapy is completed.
Male reproductive potential: Male patients whose female partners can become pregnant should be advised to use effective contraception during treatment and for 2 months after the final dose of Regorafenib.
Infertility: There are no data on the effect of Regorafenib on human fertility.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Overdose
The highest dose of Regora tested in clinical studies is 220 mg per day. At this dose, the reactions seen most often were skin problems, dysphonia, diarrhea, mucosal inflammation, dry mouth, decreased appetite, hypertension and fatigue. There is no known antidote for a Regora overdose. If an overdose is suspected, Regora should be interrupted, supportive care should be started, and the patient should be observed until their condition is stable.
⚠️ In an emergency call 999 or go to the nearest hospital emergency department.
Storage
Keep Regorafenib Monohydrate below 30°C, in a cool and dry place and away from sunlight. Keep it out of the reach of children.
Drug Interactions
Common questions about Regora 40 mg
What is Regora 40 mg Tablet?
Regora 40 mg Tablet is a medicine that contains Regorafenib Monohydrate. It is made by Beacon Pharmaceuticals PLC. It belongs to the Targeted Cancer Therapy group of medicines.
What is Regora used for?
Regorafenib Monohydrate is used to treat metastatic colorectal cancer (CRC) in patients who have already been treated with fluoropyrimidine, oxaliplatin and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if the cancer is RAS wild-type, an anti-EGFR therapy. The same use is stated again for colorectal cancer: the medicine is indicated for patients with metastatic colorectal cancer (CRC) whose earlier treatment included fluoropyrimidine, oxaliplatin and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if RAS wild-type, an anti-EGFR therapy.
What are the side effects of Regora?
Hepatotoxicity, infections, hemorrhage, gastrointestinal perforation or fistula, dermatological toxicity, hypertension, cardiac ischemia and infarction, Reversible Posterior Leukoencephalopathy Syndrome (RPLS).
Can I take Regora during pregnancy or while breastfeeding?
No data are available on the use of Regorafenib in pregnant women, but pregnant women should still be told about the possible hazard to the fetus. Nobody knows yet whether Regorafenib or its metabolites pass into human milk, what effect Regorafenib has on a breastfed infant, or whether it changes milk production. Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
What happens if I take too much Regora?
The highest dose of Regora tested in clinical studies is 220 mg per day. At this dose, the reactions seen most often were skin problems, dysphonia, diarrhea, mucosal inflammation, dry mouth, decreased appetite, hypertension and fatigue. In an emergency call 999 or go to the nearest hospital emergency department.
How should I store Regora?
Keep Regorafenib Monohydrate below 30°C, in a cool and dry place and away from sunlight. Keep it out of the reach of children.
Can I take other medicines with Regora?
Some medicines can interact with Regorafenib Monohydrate, for example: Clarithromycin, Itraconazole, Telithromycin, Voriconazole, Posaconazole, Ketoconazole. Tell your doctor or pharmacist about every medicine you take.
Is there a cheaper medicine with the same ingredient?
Regocent by Incepta Pharmaceuticals Ltd. has the same ingredient and strength for ৳200.00 per unit, compared with ৳700.00 for Regora. Ask your doctor or pharmacist before switching.
Do I need a prescription for Regora?
Regora is a prescription (Rx) medicine. Take it as your doctor advises.