Regora40 mg

Regora 40 mg is a kinase inhibitor that is indicated: For the treatment of metastatic colorectal cancer (CRC) after disease progression on or intolerance to fluoropyrimidine-based chemotherapy, anti-VEGF therapy and anti-EGFR therapy. For the treatment of unresectable or metastatic gastrointestinal stromal tumours (GIST) after disease progression on or intolerance to prior treatment with imatinib and sunitinib. ... Read moreRegora 40 mg is a kinase inhibitor that is indicated: For the treatment of metastatic colorectal cancer (CRC) after disease progression on or intolerance to fluoropyrimidine-based chemotherapy, anti-VEGF therapy and anti-EGFR therapy. For the treatment of unresectable or metastatic gastrointestinal stromal tumours (GIST) after disease progression on or intolerance to prior treatment with imatinib and sunitinib. For the treatment of hepatocellular carcinoma (HCC) in patients who have been previously treated with sorafenib

Targeted Cancer Therapy

Regora 40 mg is a small molecule inhibitor of multiple membrane-bound and intracellular kinases involved in normal cellular functions and in pathologic processes such as oncogenesis, tumor angiogenesis, metastasis and tumor immunity. In in vitro biochemical or cellular assays, Regora 40 mg 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 at concentrations of Regora 40 mg that have been achieved clinically. In in vivo models, Regora 40 mg demonstrated anti-angiogenic activity in a rat tumor model and inhibition of tumor growth in several mouse xenograft models including some for human colorectal carcinoma, gastrointestinal stromal and hepatocellular carcinoma. Regora 40 mg also demonstrated anti-metastatic activity in a mouse xenograft model and two mouse orthotopic models of human colorectal carcinoma.

Metastatic colorectal cancer (CRC): 160 mg orally, once daily for the first 21 days of each 28-day cycle.Gastrointestinal stromal tumours (GIST): 160 mg orally, once daily for the first 21 days of each 28-day cycle.Hepatocellular carcinoma (HCC): 160 mg orally, once daily for the first 21 days of each 28-day cycle.

Advise patients to swallow the Regora 40 mg tablet whole with water at the same time each day following a low-fat meal. Inform patients that the low-fat meal should contain less than 600 calories and less than 30% fatAdvise patients to store medicine in the original container. Do not place medication in daily or weekly pill boxes. Discard any remaining tablets 7 weeks after opening the bottle. Tightly close bottle after each opening and keep the desiccant in the bottle

CYP3A4 Inhibitors: Avoid concomitant use of strong CYP3A4 inhibitors with Regora 40 mg.CYP3A4 Inducers: Avoid concomitant use of strong CYP3A4 inducers with Regora 40 mg.

None

The most common side effects (≥30%) are asthenia/fatigue, decreased appetite and food intake, hand-foot skin reaction (HFSR) [palmar-plantar erythrodysesthesia (PPE)], diarrhea, mucositis, weight loss, infection, hypertension, and dysphonia.

Pregnancy: Based on animal studies and its mechanism of action, Regora 40 mg can cause fetal harm when administered to a pregnant woman. There are no available data on Regora 40 mg use in pregnant women. Administration of Regora 40 mg was embryolethal and teratogenic in rats and rabbits at exposures lower than human exposures at the recommended dose, with increased incidences of cardiovascular, genitourinary, and skeletal malformations. Advise pregnant women of the potential hazard to a fetus.The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4 % and 15 to 20%, respectively.Lactation: There are no data on the presence of Regora 40 mg or its metabolites in human milk, the effects of Regora 40 mg on the breastfed infant, or on milk production. In rats, Regora 40 mg and its metabolites are excreted in milk. Because of the potential for serious adverse reactions in breastfed infants from Regora 40 mg, do not breastfeed during treatment with Regora 40 mg and for 2 weeks after the final dose.

Hemorrhage: Permanently discontinue Regora 40 mg for severe or life-threatening hemorrhage. Dermatological toxicity: Interrupt and then reduce or discontinue Regora 40 mg depending on severity and persistence of dermatologic toxicity. Hypertension: Temporarily or permanently discontinue Regora 40 mg for severe or uncontrolled hypertension. Cardiac ischemia and infarction: Withhold Regora 40 mg for new or acute cardiac ischemia/infarction and resume only after resolution of acute ischemic events. Reversible Posterior Leukoencephalopathy Syndrome (RPLS): Discontinue Regora 40 mg. Gastrointestinal perforation or fistulae: Discontinue Regora 40 mg. Wound healing complications: Stop Regora 40 mg before surgery. Discontinue in patients with wound dehiscence. Embryofetal toxicity: Can cause fetal harm. Advise women of potential risk to a fetus.

The highest dose of Regora 40 mg studied clinically is 220 mg per day. The most frequently observed adverse drug reactions at this dose were dermatological events, dysphonia, diarrhea, mucosal inflammation, dry mouth, decreased appetite, hypertension, and fatigue. There is no known antidote for Regora 40 mg overdose. In the event of suspected overdose, interrupt Regora 40 mg, institute supportive care, and observe until clinical stabilization.

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.

Pediatric Use: The safety and efficacy of Regora 40 mg in pediatric patients less than 18 years of age have not been established.Geriatric Use: Of the 1142 Regora 40 mg-treated patients enrolled in randomized, placebo-controlled trials, 40% were 65 years of age and over, while 10% were 75 and over. No overall differences in efficacy were observed between these patients and younger patients. There was an increased incidence of Grade 3 hypertension (18% versus 9%) in the placebo-controlled trials among Regora 40 mg-treated patients 65 years of age and older as compared to younger patients. In addition, one Grade 4 hypertension event has been reported in the 65 years and older age group and none in the younger age group.Hepatic Impairment: No dose adjustment is recommended in patients with mild or moderate hepatic impairment. Closely monitor patients with hepatic impairment for adverse reactions. Regora 40 mg is not recommended for use in patients with severe hepatic impairment as Regora 40 mg has not been studied in this population.Renal Impairment: No dose adjustment is recommended for patients with renal impairment. The pharmacokinetics of Regora 40 mg have not been studied in patients who are on dialysis and there is no recommended dose for this patient population

Targeted Cancer Therapy

Regora 40 mg is a kinase inhibitor and it inhibits multiple membrane-bound and intracellular kinases involved in normal cellular functions and in pathologic processes such as oncogenesis, tumor angiogenesis, and maintenance of the tumor microenvironment. Regora 40 mg or its major human active metabolites M-2 and M-5 inhibits the activity of RET, VEGFR1, VEGFR2, VEGFR3, KIT, PDGFR-alpha, PDGFR-beta, FGFR1, FGFR2, TIE2, DDR2, Trk2A, Eph2A, RAF-1, BRAF, BRAFV600E, SAPK2, PTK5, and Abl. Due to its inhibitory functions, Regora 40 mg can inhibit the progression of certain solid tumors.

Regora 40 mg is Pregnancy Category D. Based on its mechanism of action, Regora 40 mg can cause fetal harm when administered to a pregnant woman. There are no adequate and well-controlled studies with Regora 40 mg in pregnant women. Based on animal reproduction studies Regora 40 mg was seen to cause embryo lethal and teratogenic defects and also increased the incidences of cardiovascular, genitourinary, and skeletal malformations in animals. Advice pregnant women or women with reproductive potential of the potential hazards of Regora 40 mg to the fetus. There is no information regarding the presence of Regora 40 mg or its metabolites being excreted in human milk. Regora 40 mg and its metabolites were excreted in rat milk and because of the potential for serious adverse reactions in nursing infants from Regora 40 mg, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use: The safety and effectiveness of Regora 40 mg in pediatric patients less than 18 years have not been established.Geriatric Use: No overall differences in safety or effectiveness were observed between adult subjects and younger subjects.Hepatic Impairment: No clinically important differences in the mean exposure of Regora 40 mg or the active metabolites M-2 and M-5 were observed in patients with hepatocellular carcinoma and mild (Child-Pugh A) or moderate (Child-Pugh B) hepatic impairment compared to patients with normal hepatic function. No dose adjustment is recommended in patients with mild or moderate hepatic impairment. Closely monitor patients with hepatic impairment for adverse reactions. Regora 40 mg is not recommended for use in patients with severe hepatic impairment (Child-Pugh Class C) as it has not been studied in this population.Renal Impairment: No dose adjustment is recommended for patients with mild renal impairment. Limited pharmacokinetic data are available from patients with moderate renal impairment (CLcr 30-59 mL/min/1.73m2). Regora 40 mg has not been studied in patients with severe renal impairment or end-stage renal disease.Females and Males of Reproductive Potential: Contraception: Use effective contraception during treatment and up to 2 months after completion of therapy. Infertility: There are no data on the effect of Regora 40 mg on human fertility. Results from animal studies indicate that Regora 40 mg can impair male and female fertility