#Regonat 40mg Tablets

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Regonat 40mg

Regonat 40mg is an oral multi-kinase inhibitor that marks angiogenic, stromal and oncogenic receptor tyrosine kinase (RTK). Regonat 40mg shows anti-angiogenic action due to its dual present VEGFR2-TIE2 tyrosine kinase inhibition. It is used for the medication of metastatic colorectal cancer and advanced gastrointestinal stromal tumors.

Mechanism of action:

Regonat 40mg is a small molecule determent of various membrane- obligated and intracellular kinases involved in normal cellular activity and in pathologic development such as oncogenesis, tumor angiogenesis, and preservation of the tumor micro-environment. Regonat 40mg establish anti-angiogenic action in a rat tumor form, and prevention of tumor growth as well as anti-metastatic action in various mouse xenograft models containing some for human colorectal carcinoma. Regonat 40mg synthetic or cellular estimation, Regonat 40mg or its extensive human effective metabolites M-2 and M-5 prevent the action of RET, VEGFR1, VEGFR2, VEGFR3, KIT, PDGFR-alpha, PDGFR-beta, FGFR1, FGFR2, TIE2, DDR2, TrkA, Eph2A, RAF-1, BRAF, BRAFV600E, SAPK2, PTK5, and Abl at the combination of Regonat 40mg that has been obtaining scientific.

Pharmacokinetics:

1. Absorption:

The geometric mean of peak plasma level (Cmax) is 2.5µg/mL in 4 hours for a single dose, at a steady-state is 3.9µg/mL & bioavailability of tablets is compared relatively in oral solution is 69% & 83%.

2. Distribution:

Regonat 40mg go through enterohepatic distribution with multiple plasma concentration peaks checked across the 24-hour dosing interruption.

3. Metabolism:

Regonat 40mg is metabolized by CYP3A4 and UGT1A9. (99.8% and 99.95%).It is determined to steady-state in human plasma are M-2 (N-oxide) and M-5 (N-oxide and N-dimethyl), having both of them connected pharmacological action and steady-state combination as Regonat 40mg. M-2 and M-5 are highly protein-bound.

4. Excretion:

It was almost 71% of radiolabeled dosage was excreted in via feces; it was excreted in urine is 19% within 12 days in a single dose after an oral solution.

·        M-2 active metabolite is 25 hr

·        M-5 active metabolite is 51hr

Dosage & Administration

The suggested dose is 160 mg Regonat 40mg (four 40 mg tablets) taken orally once everyday for the first 21 days of each 28­ day period.

Drug Interaction:

Regonat 40mg is a strong CYP3A4 inducer (rifampin) with a single 160 mg dose.

Regonat 40mg is a strong CYP3A4 inhibitor (ketoconazole) with a single 160 mg dose.

Side Effects:

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.

Pregnancy & lactation:

Regonat 40mg should not be used in a Pregnancy situation

No breastfeeding is suggested

Storage:

Store Regonat 40mg at 25°C (77°F). Keep the bottle hard closed.

Uses: Regonat 40mg is used to treatment of cancer to the colon and rectum.