pibrentasvir Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antivirals, hepatitis C Virus (HCV) NS5A inhibitors | 5244 | 1353900-92-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Pibrentasvir is an inhibitor of HCV NS5A, which is essential for viral RNA replication and virion assembly. The mechanism of action of pibrentasvir has been characterized based on cell culture antiviral activity and drug resistance mapping studies.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 26, 2017 | EMA | AbbVie Deutschland GmbH & Co. KG | |
| Aug. 3, 2017 | FDA | ABBVIE INC |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Headache | 977.12 | 32.60 | 630 | 4883 | 477722 | 46202827 |
| Fatigue | 971.84 | 32.60 | 687 | 4826 | 608010 | 46072539 |
| Pruritus | 471.87 | 32.60 | 313 | 5200 | 242039 | 46438510 |
| Nausea | 317.13 | 32.60 | 393 | 5120 | 687061 | 45993488 |
| Blood bilirubin increased | 95.56 | 32.60 | 56 | 5457 | 34128 | 46646421 |
| Product dose omission issue | 86.87 | 32.60 | 103 | 5410 | 168417 | 46512132 |
| Therapy cessation | 47.80 | 32.60 | 33 | 5480 | 26596 | 46653953 |
| Wrong schedule | 46.58 | 32.60 | 9 | 5504 | 150 | 46680399 |
| Jaundice | 43.17 | 32.60 | 32 | 5481 | 28813 | 46651736 |
| Rash | 40.14 | 32.60 | 112 | 5401 | 356400 | 46324149 |
| Hepatocellular carcinoma | 38.60 | 32.60 | 14 | 5499 | 2825 | 46677724 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Fatigue | 1494.91 | 28.05 | 864 | 5187 | 319809 | 29626618 |
| Headache | 1448.42 | 28.05 | 704 | 5347 | 181602 | 29764825 |
| Nausea | 226.58 | 28.05 | 287 | 5764 | 296670 | 29649757 |
| Pruritus | 156.46 | 28.05 | 153 | 5898 | 118051 | 29828376 |
| Hepatocellular carcinoma | 95.40 | 28.05 | 44 | 6007 | 9566 | 29936861 |
| Blood bilirubin increased | 71.10 | 28.05 | 59 | 5992 | 36577 | 29909850 |
| Product dose omission issue | 64.98 | 28.05 | 86 | 5965 | 91545 | 29854882 |
| Hepatic cirrhosis | 63.97 | 28.05 | 40 | 6011 | 15959 | 29930468 |
| Therapy cessation | 58.40 | 28.05 | 37 | 6014 | 15100 | 29931327 |
| Abdominal discomfort | 53.07 | 28.05 | 57 | 5994 | 48734 | 29897693 |
| Hepatitis C | 52.75 | 28.05 | 33 | 6018 | 13172 | 29933255 |
| Child-Pugh-Turcotte score increased | 36.55 | 28.05 | 7 | 6044 | 62 | 29946365 |
| Diarrhoea | 36.24 | 28.05 | 148 | 5903 | 333955 | 29612472 |
| Viral load increased | 34.48 | 28.05 | 15 | 6036 | 2839 | 29943588 |
| Jaundice | 31.91 | 28.05 | 36 | 6015 | 32450 | 29913977 |
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 | 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 EPC | N0000191256 | Hepatitis C Virus NS5A Inhibitor |
| FDA MoA | N0000191272 | UGT1A1 Inhibitors |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Chronic hepatitis C | indication | 128302006 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 11.04 | acidic |
| pKa2 | 11.64 | acidic |
| pKa3 | 12.69 | acidic |
| pKa4 | 13.29 | acidic |
| pKa5 | 5.17 | Basic |
| pKa6 | 4.56 | Basic |
| pKa7 | 1.2 | Basic |
Orange Book patent data (new drug applications)
None
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 INC | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | Aug. 6, 2021 | REVISIONS TO THE GLECAPREVIR/PIBRENTASVIR COMBINULLTION PRODUCT PRESCRIBING INFORMATION TO INCLUDE SAFETY AND EFFICACY DATA FROM THE HCV/HIV-1 COINFECTION STUDY M14-730 AND FROM THE LIVER AND RENULLL TRANSPLANT STUDY M13-596 |
| 100MG;40MG | MAVYRET | ABBVIE INC | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | April 30, 2022 | NEW PATIENT POPULATION |
| 100MG;40MG | MAVYRET | ABBVIE INC | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | Aug. 3, 2022 | NEW CHEMICAL ENTITY |
| 100MG;40MG | MAVYRET | ABBVIE INC | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | Sept. 26, 2022 | EIGHT-WEEK DOSING REGIMEN FOR THE TREATMENT OF GENOTYPES 1, 2, 3, 4, 5, AND 6, CHRONIC HEPATITIS C VIRUS INFECTION IN TREATMENT-NULLIVE SUBJECTS WITH COMPENSATED CIRRHOSIS BASED ON THE RESULTS FROM THE EXPEDITION-8 STUDY |
| 100MG;40MG | MAVYRET | ABBVIE INC | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | Oct. 30, 2022 | PEDIATRIC EXCLUSIVITY |
| 100MG;40MG | MAVYRET | ABBVIE INC | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | Feb. 3, 2023 | PEDIATRIC EXCLUSIVITY |
| 100MG;40MG | MAVYRET | ABBVIE INC | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | March 26, 2023 | PEDIATRIC EXCLUSIVITY |
| 100MG;40MG | MAVYRET | ABBVIE INC | 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 |
| 100MG;40MG | MAVYRET | ABBVIE INC | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | Oct. 10, 2023 | PEDIATRIC EXCLUSIVITY |
| 100MG;40MG | MAVYRET | ABBVIE INC | 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 INC | 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 INC | N209394 | Aug. 3, 2017 | RX | TABLET | ORAL | Oct. 30, 2026 | PEDIATRIC EXCLUSIVITY |
Bioactivity Summary:
None
External reference:
| ID | Source |
|---|---|
| 4036872 | VANDF |
| C4310001 | UMLSCUI |
| CHEMBL3545123 | ChEMBL_ID |
| 58031952 | PUBCHEM_CID |
| D10816 | KEGG_DRUG |
| DB13878 | DRUGBANK_ID |
| C000612854 | MESH_SUPPLEMENTAL_RECORD_UI |
| 11268 | IUPHAR_LIGAND_ID |
| C000622691 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10260 | INN_ID |
| 2WU922TK3L | UNII |
| 1940636 | RXNORM |
| 33001 | MMSL |
| d08634 | MMSL |
| 017296 | NDDF |
| 736836002 | SNOMEDCT_US |
| 816102004 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Mavyret | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0074-2600 | PELLET | 20 mg | ORAL | NDA | 32 sections |
| Mavyret | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0074-2625 | TABLET, FILM COATED | 40 mg | ORAL | NDA | 32 sections |