glecaprevir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| Hepatitis Virus C (HVC) protease inhibitors | 5243 | 1365970-03-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Glecaprevir is an inhibitor of the HCV NS3/4A protease, which is necessary for the proteolytic cleavage of the HCV encoded polyprotein (into mature forms of the NS3, NS4A, NS4B, NS5A, and NS5B proteins) and is essential for viral replication. In a biochemical assay, glecaprevir inhibited the proteolytic activity of recombinant NS3/4A enzymes from clinical isolates of HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, and 6a with IC50 values ranging from 3.5 to 11.3 nM.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 4 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 26, 2017 | EMA | AbbVie Deutschland GmbH & Co. KG | |
| Aug. 3, 2017 | FDA | ABBVIE INC | |
| Sept. 27, 2017 | PMDA | AbbVie GK |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J05AP57 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HCV infections |
| FDA MoA | N0000182138 | Cytochrome P450 1A2 Inhibitors |
| FDA MoA | N0000182638 | HCV NS3/4A Protease Inhibitors |
| FDA EPC | N0000182639 | Hepatitis C Virus NS3/4A Protease Inhibitor |
| FDA MoA | N0000185503 | P-Glycoprotein Inhibitors |
| FDA MoA | N0000190107 | Organic Anion Transporting Polypeptide 1B1 Inhibitors |
| FDA MoA | N0000190108 | Organic Anion Transporting Polypeptide 1B3 Inhibitors |
| FDA MoA | N0000190113 | Breast Cancer Resistance Protein Inhibitors |
| FDA MoA | N0000190114 | Cytochrome P450 3A Inhibitors |
| FDA MoA | N0000191272 | UGT1A1 Inhibitors |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Chronic hepatitis C | indication | 128302006 | |
| Compensated cirrhosis | indication | 371139006 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.64 | acidic |
| pKa2 | 0.86 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 100MG;40MG | MAVYRET | ABBVIE | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | 10028937 | June 10, 2030 | TREATMENT OF CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1, 2, 3, 4, 5, OR 6 |
| 100MG;40MG | MAVYRET | ABBVIE | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | 10028937 | June 10, 2030 | TREATMENT OF CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1, 2, 3, 4, 5, OR 6 IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER OR WEIGHING AT LEAST 45 KG |
| 100MG;40MG | MAVYRET | ABBVIE | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | 10039754 | June 10, 2030 | TREATMENT OF CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1, 2, 3, 4, 5, OR 6 |
| 100MG;40MG | MAVYRET | ABBVIE | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | 10039754 | June 10, 2030 | TREATMENT OF CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1, 2, 3, 4, 5, OR 6 IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER OR WEIGHING AT LEAST 45 KG |
| 50MG;20MG/PACKET | MAVYRET | ABBVIE | N215110 | June 10, 2021 | RX | PELLETS | ORAL | 10028937 | June 10, 2030 | TREATMENT OF CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1, 2, 3, 4, 5, OR 6 IN PEDIATRIC PATIENTS 3 TO LESS THAN 12 YEARS OF AGE OR WEIGHING LESS THAN 45 KG |
| 50MG;20MG/PACKET | MAVYRET | ABBVIE | N215110 | June 10, 2021 | RX | PELLETS | ORAL | 10039754 | June 10, 2030 | TREATMENT OF CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1, 2, 3, 4, 5, OR 6 IN PEDIATRIC PATIENTS 3 TO LESS THAN 12 YEARS OF AGE OR WEIGHING LESS THAN 45 KG |
| 100MG;40MG | MAVYRET | ABBVIE | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | 9586978 | Nov. 6, 2030 | TREATMENT OF CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1, 2, 3, 4, 5, OR 6 |
| 100MG;40MG | MAVYRET | ABBVIE | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | 9586978 | Nov. 6, 2030 | TREATMENT OF CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1, 2, 3, 4, 5, OR 6 IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER OR WEIGHING AT LEAST 45 KG |
| 50MG;20MG/PACKET | MAVYRET | ABBVIE | N215110 | June 10, 2021 | RX | PELLETS | ORAL | 9586978 | Nov. 6, 2030 | TREATMENT OF CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1, 2, 3, 4, 5, OR 6 IN PEDIATRIC PATIENTS 3 TO LESS THAN 12 YEARS OF AGE OR WEIGHING LESS THAN 45 KG |
| 100MG;40MG | MAVYRET | ABBVIE | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | 8648037 | Jan. 19, 2032 | TREATMENT OF CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1, 2, 3, 4, 5, OR 6 |
| 100MG;40MG | MAVYRET | ABBVIE | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | 8648037 | Jan. 19, 2032 | TREATMENT OF CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1, 2, 3, 4, 5, OR 6 IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER OR WEIGHING AT LEAST 45 KG |
| 50MG;20MG/PACKET | MAVYRET | ABBVIE | N215110 | June 10, 2021 | RX | PELLETS | ORAL | 8648037 | Jan. 19, 2032 | TREATMENT OF CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1, 2, 3, 4, 5, OR 6 IN PEDIATRIC PATIENTS 3 TO LESS THAN 12 YEARS OF AGE OR WEIGHING LESS THAN 45 KG |
| 100MG;40MG | MAVYRET | ABBVIE | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | 10286029 | March 14, 2034 | TREATMENT OF CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1, 2, 3, 4, 5, OR 6 IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER OR WEIGHING AT LEAST 45 KG |
| 100MG;40MG | MAVYRET | ABBVIE | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | 11484534 | March 14, 2034 | TREATMENT OF CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1, 2, 3, 4, 5, OR 6 IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER OR WEIGHING AT LEAST 45 KG |
| 50MG;20MG/PACKET | MAVYRET | ABBVIE | N215110 | June 10, 2021 | RX | PELLETS | ORAL | 10286029 | March 14, 2034 | TREATMENT OF CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1, 2, 3, 4, 5, OR 6 IN PEDIATRIC PATIENTS 3 TO LESS THAN 12 YEARS OF AGE OR WEIGHING LESS THAN 45 KG |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 100MG;40MG | MAVYRET | ABBVIE | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | Feb. 3, 2023 | PEDIATRIC EXCLUSIVITY |
| 50MG;20MG/PACKET | MAVYRET | ABBVIE | N215110 | June 10, 2021 | RX | PELLETS | ORAL | Feb. 3, 2023 | PEDIATRIC EXCLUSIVITY |
| 100MG;40MG | MAVYRET | ABBVIE | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | March 26, 2023 | PEDIATRIC EXCLUSIVITY |
| 50MG;20MG/PACKET | MAVYRET | ABBVIE | N215110 | June 10, 2021 | RX | PELLETS | ORAL | March 26, 2023 | PEDIATRIC EXCLUSIVITY |
| 100MG;40MG | MAVYRET | ABBVIE | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | April 10, 2023 | INFORMATION ADDED TO THE LABELING REGARDING SAFETY AND EFFICACY IN SUBJECTS WITH HCV SUBTYPE 3B INFECTION |
| 50MG;20MG/PACKET | MAVYRET | ABBVIE | N215110 | June 10, 2021 | RX | PELLETS | ORAL | April 10, 2023 | INFORMATION ADDED TO THE LABELING REGARDING SAFETY AND EFFICACY IN SUBJECTS WITH HCV SUBTYPE 3B INFECTION |
| 100MG;40MG | MAVYRET | ABBVIE | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | Oct. 10, 2023 | PEDIATRIC EXCLUSIVITY |
| 50MG;20MG/PACKET | MAVYRET | ABBVIE | N215110 | June 10, 2021 | RX | PELLETS | ORAL | Oct. 10, 2023 | PEDIATRIC EXCLUSIVITY |
| 100MG;40MG | MAVYRET | ABBVIE | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | April 30, 2026 | TREATMENT OF PEDIATRIC PATIENTS 12 YEARS AND OLDER OR WEIGHING AT LEAST 45 KG WITH CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1,2,3,4,5 OR 6 INFECTION WITHOUT CIRRHOSIS OR WITH COMPENSATED CIRRHOSIS (CHILD-PUGH A) |
| 100MG;40MG | MAVYRET | ABBVIE | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | April 30, 2026 | TREATMENT OF PEDIATRIC PATIENTS 12 YEARS AND OLDER OR WEIGHING AT LEAST 45 KG WITH HCV GENOTYPE 1 INFECTION, WHO PREVIOUSLY HAVE BEEN TREATED WITH A REGIMEN CONTAINING AN HCV NS5A INHIBITOR OR AN NS3/4A PROTEASE INHIBITOR (PI), BUT NOT BOTH |
| 100MG;40MG | MAVYRET | ABBVIE | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | Oct. 30, 2026 | PEDIATRIC EXCLUSIVITY |
| 100MG;40MG | MAVYRET | ABBVIE | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | June 10, 2028 | FOR TREATMENT OF PEDIATRIC PATIENTS 3 YEARS OF AGE TO LESS THAN 12 YEARS OF AGE WEIGHING LESS THAN 45 KG WITH CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1, 2, 3, 4, 5 OR 6 INFECTION WITHOUT CIRRHOSIS OR WITH COMPENSATED CIRRHOSIS (CHILD-PUGH A); AND TREATMENT OF PEDIATRIC PATIENTS 3 YEARS OF AGE TO LESS THAN 12 YEARS OF AGE WEIGHING LESS THAN 45 KG WITH HCV GENOTYPE 1 INFECTION, WHO PREVIOUSLY HAVE BEEN TREATED WITH A REGIMEN CONTAINING AN HCV NS5A INHIBITOR OR AN NS3/4A PROTEASE INHIBITOR (PI), B |
| 50MG;20MG/PACKET | MAVYRET | ABBVIE | N215110 | June 10, 2021 | RX | PELLETS | ORAL | June 10, 2028 | FOR TREATMENT OF PEDIATRIC PATIENTS 3 YEARS OF AGE TO LESS THAN 12 YEARS OF AGE WEIGHING LESS THAN 45 KG WITH CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1, 2, 3, 4, 5 OR 6 INFECTION WITHOUT CIRRHOSIS OR WITH COMPENSATED CIRRHOSIS (CHILD-PUGH A); AND TREATMENT OF PEDIATRIC PATIENTS 3 YEARS OF AGE TO LESS THAN 12 YEARS OF AGE WEIGHING LESS THAN 45 KG WITH HCV GENOTYPE 1 INFECTION, WHO PREVIOUSLY HAVE BEEN TREATED WITH A REGIMEN CONTAINING AN HCV NS5A INHIBITOR OR AN NS3/4A PROTEASE INHIBITOR (PI), B |
| 100MG;40MG | MAVYRET | ABBVIE | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | Dec. 10, 2028 | PEDIATRIC EXCLUSIVITY |
| 50MG;20MG/PACKET | MAVYRET | ABBVIE | N215110 | June 10, 2021 | RX | PELLETS | ORAL | Dec. 10, 2028 | PEDIATRIC EXCLUSIVITY |
Bioactivity Summary:
None
External reference:
| ID | Source |
|---|---|
| K6BUU8J72P | UNII |
| 4036871 | VANDF |
| C4519536 | UMLSCUI |
| O31 | PDB_CHEM_ID |
| CHEMBL3545363 | ChEMBL_ID |
| 66828839 | PUBCHEM_CID |
| DB13879 | DRUGBANK_ID |
| D10814 | KEGG_DRUG |
| 10261 | INN_ID |
| 11267 | IUPHAR_LIGAND_ID |
| 33000 | MMSL |
| d08633 | MMSL |
| 017295 | NDDF |
| 736837006 | SNOMEDCT_US |
| 816101006 | SNOMEDCT_US |
| 1940635 | RXNORM |
| C000612853 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Mavyret | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0074-2600 | PELLET | 50 mg | ORAL | NDA | 34 sections |
| Mavyret | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0074-2600 | PELLET | 50 mg | ORAL | NDA | 34 sections |
| Mavyret | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0074-2600 | PELLET | 50 mg | ORAL | NDA | 34 sections |
| Mavyret | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0074-2625 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 34 sections |
| Mavyret | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0074-2625 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 34 sections |
| Mavyret | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0074-2625 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 34 sections |