Ledipasvir

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Ledipasvir

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Catalog Number	PR1256388518
CAS	1256388-51-8
Description	Ledipasvir is a Hepatitis C Virus NS5A Inhibitor. The mechanism of action of ledipasvir is as a P-Glycoprotein Inhibitor, and Breast Cancer Resistance Protein Inhibitor.
Synonyms	Ledipasvir acetonate; GS 5885
IUPAC Name	methyl N-[(2S)-1-[(6S)-6-[5-[9,9-difluoro-7-[2-[(1R,3S,4S)-2-[(2S)-2-(methoxycarbonylamino)-3-methylbutanoyl]-2-azabicyclo[2.2.1]heptan-3-yl]-3H-benzimidazol-5-yl]fluoren-2-yl]-1H-imidazol-2-yl]-5-azaspiro[2.4]heptan-5-yl]-3-methyl-1-oxobutan-2-yl]carbamate
Molecular Weight	889.0
Molecular Formula	C49H54F2N8O6
InChI	VRTWBAAJJOHBQU-KMWAZVGDSA-N
InChI Key	InChI=1S/C49H54F2N8O6/c1-24(2)39(56-46(62)64-5)44(60)58-23-48(15-16-48)21-38(58)42-52-22-37(55-42)28-9-13-32-31-12-8-26(18-33(31)49(50,51)34(32)19-28)27-10-14-35-36(20-27)54-43(53-35)41-29-7-11-30(17-29)59(41)45(61)40(25(3)4)57-47(63)65-6/h8-10,12-14,18-20,22,24-25,29-30,38-41H,7,11,15-17,21,23H2,1-6H3,(H,52,55)(H,53,54)(H,56,62)(H,57,63)/t29-,30+,38-,39-,40-,41-/m0/s1
Drug Categories	Anti-Infective Agents; Antiinfectives for Systemic Use; Antiviral Agents; Antivirals for Systemic Use; Antivirals for treatment of HCV infections; BCRP/ABCG2 Inhibitors; Direct Acting Antivirals; Drugs that are Mainly Renally Excreted; Hepatitis C Virus NS5A Inhibitor; Heterocyclic Compounds, Fused-Ring; P-glycoprotein inhibitors; P-glycoprotein substrates; Treatments for Hepatitis C
Drug Interactions	Abacavir-Abacavir may decrease the excretion rate of Ledipasvir which could result in a higher serum level. Abemaciclib-The serum concentration of Abemaciclib can be increased when it is combined with Ledipasvir. Abrocitinib-The serum concentration of Ledipasvir can be increased when it is combined with Abrocitinib. Aceclofenac-Aceclofenac may decrease the excretion rate of Ledipasvir which could result in a higher serum level. Acemetacin-Acemetacin may decrease the excretion rate of Ledipasvir which could result in a higher serum level.
Isomeric SMILES	CC(C)[C@@H](C(=O)N1CC2(CC2)C[C@H]1C3=NC=C(N3)C4=CC5=C(C=C4)C6=C(C5(F)F)C=C(C=C6)C7=CC8=C(C=C7)N=C(N8)[C@@H]9[C@H]1CC[C@H](C1)N9C(=O)[C@H](C(C)C)NC(=O)OC)NC(=O)OC
Standard	In-house
Type	Small Molecule

Pharmacology

Indications

Ledipasvir, when utilized in conjunction with the antiviral medication sofosbuvir, is primarily indicated for the treatment of chronic hepatitis C virus (HCV) infection in both adult and pediatric patients who are 3 years of age and older. This combination therapy is effective in cases with specified conditions of HCV infection. Furthermore, ledipasvir has demonstrated efficacy in treating HCV among patients who are co-infected with the human immunodeficiency virus (HIV).

Pharmacodynamics

Ledipasvir functions as a direct-acting antiviral agent (DAA) against the hepatitis C virus. It is designed to target and disrupt specific stages of the viral replication process. Importantly, even at a high dose of 120 mg twice daily, which is 2.67 times the maximum recommended dosage, ledipasvir does not result in any clinically significant prolongation of the QTc interval, ensuring its safety from a cardiac perspective.

Absorption

Upon oral administration, ledipasvir attains its peak plasma concentration within approximately 4 to 4.5 hours, achieving a maximum concentration (Cmax) of 323 ng/mL. This pharmacokinetic profile is crucial for determining the timing and effectiveness of the drug's therapeutic action in patients undergoing treatment for HCV infection.

Metabolism

In terms of metabolism, ledipasvir shows a distinctive profile. In vitro studies indicate that ledipasvir is not metabolized by human CYP enzymes, including CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. Although there is evidence of a slow oxidative metabolism through an unidentified mechanism, the drug's systemic exposure following a single 90 mg dose of [14C]-ledipasvir is predominantly to the parent compound (>98%). Additionally, the major form of ledipasvir excreted in feces remains unchanged, highlighting the drug's stability and persistence in its original form within the system.

Mechanism of Action

Ledipasvir functions as an inhibitor of the Hepatitis C Virus (HCV) NS5A protein, a critical component essential for viral RNA replication and the assembly of HCV virions. Although its precise mechanism of action has not been fully elucidated, it is suggested that Ledipasvir plays a role in preventing the hyperphosphorylation of NS5A, a process necessary for the production of viral particles. This inhibition is a key factor in its therapeutic efficacy against HCV.

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