Velakast (Sofosbuvir + Velpatasvir) 400+100 mg 28 tab

Velakast is the latest drug velpatasvir + sofosbuvir for the treatment of all genotypes of hepatitis C. The manufacturer is the well—known Indian pharmaceutical company Natco Pharma Limited. Velpatasvir Velakast is available under the trademark Aprazer Healthcare.

Composition

Velacast is an oral tablet with a fixed dosage of Sofosbuvir and velpatasvir.

Each Velakast tablet contains 400 mg of sofosbuvir and 100 mg of velpatasvir. Sofosbuvir is a nucleotide analog of the HCV NS5B polymerase inhibitor, and velpatasvir is an NS5A inhibitor.

The tablets include the following inactive ingredients: copovidone, croscarmellose sodium, magnesium stearate and microcrystalline cellulose.

The tablets are coated with a film containing the following inactive ingredients: titanium dioxide IP and diamond blue FCF, polyethylene glycol, polyvinyl alcohol, talc and titanium dioxide.

The effect of the drug

Due to its powerful composition, Velakast APRAZER Health Care is widely used to combat hepatitis C virus genotypes 1-6. The drug can be prescribed as monotherapy or for combined treatment of patients with or without cirrhosis.

The high effectiveness of the drug against all HCV genotypes is due to the presence in its composition:

Sofosbuvir: The IUPAC name (according to the nomenclature of the International Union of Theoretical and Applied Chemistry) for sofosbuvir is (S) -isopropyl 2 - ((S) - ((2R, 3R, 4R, 5R) -5 (2,4-dioxo-3,4-dihydropyrimidine-1 (2H) -yl) -4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-yl) methoxy (phenoxy) phosphorylamino) -propanoate. It has the molecular formula C22H29FN3O9P and a molecular weight of 529.45 g. Sofosbuvir is a white to almost white crystalline solid with a solubility of at least 2 mg/ml in the pH range 2-7.7 at 37 °C, slightly soluble in water.

Velpatasvir: The IUPAC name for velpatasvir is methyl {(1R) -2 - [(2S, 4S) -2- (5- {2 [( 2S, 5S) -1 - {(2S) -2 - [(methoxycarbonyl) amino] -3-methylbutanoyl} -5-methylpyrrolidine-2-il] 1,11-dihydro [2] benzopyrano [4', 3': 6,7] naphtho [1,2-d] imidazole-9-yl} -1H-imidazole-2-yl) -4 (methoxymethyl) pyrrolidine-1-yl] -2-oxo-1-phenylethyl} carbamate. It has the molecular formula C49H54N8O8 and a molecular weight of 883.0. Velpatasvir is practically insoluble (less than 0.1 mg/ml) above pH 5, slightly soluble (3.6 mg/ml) at pH 2 and soluble (more than 36mg/ml) at pH 1.2.

VELAKAST consists of a fixed dose combination of sofosbuvir and velpatasvir, which are antiviral drugs with direct action against hepatitis C virus.

Sofosbuvir is an inhibitor of HCV NS5B RNA-dependent RNA polymerase, which is necessary for virus replication. Sofosbuvir is a prodrug of nucleotides that undergoes intracellular metabolism to form a pharmacologically active uridine triphosphate analog (GS-461203), which can be incorporated into HCV RNA using NS5B polymerase and acts as a chain limiter. In biochemical analysis, GS-461203 inhibited the polymerase activity of recombinant NS5B from HCV genotypes 1b, 2a, 3a and 4a with an IC50 value in the range from 0.36 to 3.3 micromoles. GS-461203 is neither an inhibitor of human DNA and RNA polymerases, nor an inhibitor of mitochondrial RNA polymerase.

Velpatasvir is an inhibitor of HCV NS5A protein, which is necessary for virus replication. The choice of resistance in cell culture and cross—resistance studies indicates that the goal of velpatasvir is to suppress NS5A replication.

Method of application

The recommended dosage of VELAKAST is 1 tablet, taken orally once a day with or without food.

Velpatasvir is not recommended for patients with severe renal insufficiency (estimated glomerular filtration rate [eGFR] less than 30 ml/min / 1.73 m2) or with end-stage renal insufficiency (ESRD), due to higher exposure (up to 20 times) of the predominant metabolite sofosbuvir.

Velacast is indicated for the treatment of adult patients with chronic hepatitis C virus genotypes 1, 2, 3, 4, 5 or 6

without cirrhosis or with compensated cirrhosis,

with decompensated chronic cirrhosis in combination with ribavirin.

Contraindications

VELAKAST and ribavirin should not be prescribed to patients who are contraindicated with ribavirin.

Safety precautions

It is strongly not recommended to use amiodarone in conjunction with VELAKAST. For patients taking amiodarone who do not have other alternative treatments:

Consult your doctor about the risk of symptomatic bradycardia.

It is recommended to monitor the heart in an inpatient setting during the first 48 hours of HTP, after which outpatient or self-monitoring of heart rate should be performed daily, at least for the first 2 weeks of treatment.