Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C49H54F2N8O6.C4H6O6 |
| Molecular Weight | 1039.0867 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 8 / 8 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O[C@@H]([C@H](O)C(O)=O)C(O)=O.COC(=O)N[C@@H](C(C)C)C(=O)N1CC2(CC2)C[C@H]1C3=NC=C(N3)C4=CC=C5C(=C4)C(F)(F)C6=C5C=CC(=C6)C7=CC8=C(C=C7)N=C(N8)[C@@H]9[C@H]%10CC[C@H](C%10)N9C(=O)[C@@H](NC(=O)OC)C(C)C
InChI
InChIKey=ZQVLPYMRXLPMDX-KEAIDYLOSA-N
InChI=1S/C49H54F2N8O6.C4H6O6/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;5-1(3(7)8)2(6)4(9)10/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);1-2,5-6H,(H,7,8)(H,9,10)/t29-,30+,38-,39-,40-,41-;1-,2-/m00/s1
DescriptionCurator's Comment: description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/?term=23384816; http://www.ncbi.nlm.nih.gov/pubmed/?term=22314425
Curator's Comment: description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/?term=23384816; http://www.ncbi.nlm.nih.gov/pubmed/?term=22314425
Ledipasvir is an inhibitor of the Hepatitis C Virus (HCV) NS5A protein required for viral RNA replication and assembly of HCV virions. Approved in October 2014 by the FDA, ledipasvir and sofosbuvir (tradename Harvoni) are direct-acting antiviral agents indicated for the treatment of HCV genotype 1 with or without cirrhosis.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3307224 |
141.0 nM [EC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | HARVONI Approved UseIndicated for the treatment of patients with chronic hepatitis C virus (HCV) genotype 1, 4, 5, or 6 infection Launch Date2014 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
531 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31220349/ |
45 mg 1 times / day multiple, oral dose: 45 mg route of administration: Oral experiment type: MULTIPLE co-administered: [NO STEREO] PSI-7851|[NO STEREO] SOFOSBUVIR |
[NO STEREO] LEDIPASVIR plasma | Homo sapiens population: UNHEALTHY age: CHILD sex: FEMALE / MALE food status: FED |
|
323 ng/mL |
90 mg 1 times / day steady-state, oral dose: 90 mg route of administration: Oral experiment type: STEADY-STATE co-administered: [NO STEREO] PSI-7851|[NO STEREO] SOFOSBUVIR |
[NO STEREO] LEDIPASVIR plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
9320 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31220349/ |
45 mg 1 times / day multiple, oral dose: 45 mg route of administration: Oral experiment type: MULTIPLE co-administered: [NO STEREO] PSI-7851|[NO STEREO] SOFOSBUVIR |
[NO STEREO] LEDIPASVIR plasma | Homo sapiens population: UNHEALTHY age: CHILD sex: FEMALE / MALE food status: FED |
|
7290 ng × h/mL |
90 mg 1 times / day steady-state, oral dose: 90 mg route of administration: Oral experiment type: STEADY-STATE co-administered: [NO STEREO] PSI-7851|[NO STEREO] SOFOSBUVIR |
[NO STEREO] LEDIPASVIR plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
47 h |
90 mg 1 times / day steady-state, oral dose: 90 mg route of administration: Oral experiment type: STEADY-STATE co-administered: [NO STEREO] PSI-7851|[NO STEREO] SOFOSBUVIR |
[NO STEREO] LEDIPASVIR plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.2% |
90 mg 1 times / day steady-state, oral dose: 90 mg route of administration: Oral experiment type: STEADY-STATE co-administered: [NO STEREO] PSI-7851|[NO STEREO] SOFOSBUVIR |
[NO STEREO] LEDIPASVIR plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Interferon-free therapy for hepatitis C: The hurdles amid a golden era. | 2015-09 |
|
| Treatment with ledipasvir and sofosbuvir improves patient-reported outcomes: Results from the ION-1, -2, and -3 clinical trials. | 2015-06 |
|
| Fixed-dose combination of sofosbuvir and ledipasvir for the treatment of chronic hepatitis C genotype 1. | 2015-04 |
|
| Virologic response following combined ledipasvir and sofosbuvir administration in patients with HCV genotype 1 and HIV co-infection. | 2015-02-24 |
|
| Ledipasvir and sofosbuvir: Interferon free therapy for hepatitis C virus genotype 1 infection. | 2015-02-12 |
|
| Changing the face of hepatitis C management - the design and development of sofosbuvir. | 2015 |
|
| Ledipasvir : a novel synthetic antiviral for the treatment of HCV infection. | 2014-04 |
Patents
Sample Use Guides
One tablet (90 mg of ledipasvir and 400 mg of sofosbuvir) taken orally once daily with or without food. Recommended treatment duration: treatment-naive with or without cirrhosis: 12 week. Treatment-experienced without cirrhosis: 12 weeks. Treatment-experienced with cirrhosis: 24 weeks. A dose recommendation cannot be made for patients with severe renal impairment or end stage renal disease.
Route of Administration:
Oral
| Name | Type | Language | ||
|---|---|---|---|---|
|
Common Name | English | ||
|
Preferred Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
1502654-87-6
Created by
admin on Wed Apr 02 11:36:54 GMT 2025 , Edited by admin on Wed Apr 02 11:36:54 GMT 2025
|
NON-SPECIFIC STOICHIOMETRY | |||
|
RT680T6HCQ
Created by
admin on Wed Apr 02 11:36:54 GMT 2025 , Edited by admin on Wed Apr 02 11:36:54 GMT 2025
|
PRIMARY | |||
|
1499193-68-8
Created by
admin on Wed Apr 02 11:36:54 GMT 2025 , Edited by admin on Wed Apr 02 11:36:54 GMT 2025
|
PRIMARY | |||
|
78357794
Created by
admin on Wed Apr 02 11:36:54 GMT 2025 , Edited by admin on Wed Apr 02 11:36:54 GMT 2025
|
PRIMARY |
ACTIVE MOIETY
SUBSTANCE RECORD
