Velakast

VELAKAST is a fixed-dose combination tablet containing sofosbuvir and velpatasvir for oral administration. Sofosbuvir is a nucleotide analog HCV NS5B polymerase inhibitor and velpatasvir is an NS5A inhibitor. Each tablet contains 400 mg sofosbuvir and 100 mg velpatasvir. The tablets include the following inactive ingredients: copovidone, croscarmellose sodium, magnesium stearate, and microcrystalline cellulose. The tablets are film-coated with a coating material containing the following inactive ingredients: Titanium Dioxide IP and Brilliant Blue FCF, polyethylene glycol, polyvinyl alcohol, talc, and titanium dioxide.


Description

VELAKAST is a fixed-dose combination tablet containing sofosbuvir and velpatasvir for oral administration. Sofosbuvir is a nucleotide analog HCV NS5B polymerase inhibitor and velpatasvir is an NS5A inhibitor. Each tablet contains 400 mg sofosbuvir and 100 mg velpatasvir. The tablets include the following inactive ingredients: copovidone, croscarmellose sodium, magnesium stearate, and microcrystalline cellulose. The tablets are film-coated with a coating material containing the following inactive ingredients: Titanium Dioxide IP and Brilliant Blue FCF, polyethylene glycol, polyvinyl alcohol, talc, and titanium dioxide.

Effect of the drug

Thanks to the powerful composition of the drug, Velakast APRAZER HEALTHCARE is widely used to fight the hepatitis C virus of genotypes 1-6. The drug may be given as a monotherapy or for combined treatment with or without cirrhosis. The high effectiveness of the drug against all genotypes of HCV is due to the presence in its composition:

Sofosbuvir: The IUPAC name for sofosbuvir is (S)-Isopropyl 2-((S)-(((2R,3R,4R,5R)-5(2,4-dioxo-3,4-dihydropyrimidin- 1(2H)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran- 2yl)methoxy  (phenoxy)phosphorylamino)propanoate. It has a molecular formula of C22H29FN3 O9 P and a molecular weight of 529.45. Sofosbuvir is a white to off-white crystalline solid with a solubility of at least 2 mg/mL across the pH range of 2–7.7 at 37°C and is 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-methylpyrrolidin-2-yl]1,11-dihydro[2]benzopyrano[4′,3′:6,7]naphtho[1,2-d]imidazol-9- yl}-1H-imidazol-2-yl)-4(methoxymethyl)pyrrolidin-1-yl]-2-oxo-1-phenylethyl}carbamate. It has a molecular formula of C49H54 N8 O8 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 (greater than 36 mg/mL) at pH 1.2.

Mechanism of Action

VELAKAST is a fixed-dose combination of sofosbuvir and velpatasvir which are direct-acting antiviral agents against the hepatitis C virus Sofosbuvir is an inhibitor of the HCV NS5B RNA-dependent RNA polymerase, which is required for viral replication. Sofosbuvir is a nucleotide prodrug that undergoes intracellular metabolism to form the pharmacologically active uridine analog triphosphate (GS-461203), which can be incorporated into HCV RNA by the NS5B polymerase and acts as a chain terminator. In a biochemical assay, GS-461203 inhibited the polymerase activity of the recombinant NS5B from HCV genotype 1b, 2a, 3a and 4a with an IC50 value ranging from 0.36 to 3.3 micromolar. GS-461203 is neither an inhibitor of human DNA and RNA polymerases nor an inhibitor of mitochondrial RNA polymerase. Velpatasvir is an inhibitor of the HCV NS5A protein, which is required for viral replication. Resistance selection in cell culture and cross-resistance studies indicates velpatasvir targets NS5A as its mode of action.

OVERDOSAGE

No specific antidote is available for overdose with VELAKAST. If overdose occurs the patient must be monitored for evidence of toxicity. Treatment of overdose with VELAKAST consists of general supportive measures including monitoring of vital signs as well as observation of the clinical status of the patient. Hemodialysis can efficiently remove the predominant circulating metabolite of sofosbuvir, GS-331007, with an extraction ratio of 53%. Hemodialysis is unlikely to result in significant removal of velpatasvir since velpatasvir is highly bound to plasma protein.

HOW SUPPLIED AND STORAGE

Each bottle contains 28 tablets and is closed with a child-resistant closure. Storage: Store below 30°C

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