famciclovir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antivirals bicyclic heterocycle compounds | 1128 | 104227-87-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An aminopurine derivative and prodrug of penciclovir which is a competitive inhibitor of herpes simplex 2 DNA polymerase. It is used to treat HERPES SIMPLEX VIRUS INFECTION.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.75 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 250 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 77.80 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 77 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.153 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 2.254 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 10.351 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 110.154 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 93.690 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 90.980 | % | High | 1 |
| herg | hERG pIC50 | 4.140 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 891.251 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 243.781 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 93.170 | % | High | 1 |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 15.631 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 445.656 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 95.450 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 5.272 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 92.800 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 116.950 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 98.300 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 95.310 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 928.966 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 16, 2008 | PMDA | ASAHI KASEI PHARMA CORPORATION | |
| June 29, 1994 | FDA | NOVARTIS |
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 |
|---|---|---|---|---|---|---|
| Aplastic anaemia | 39.36 | 19.26 | 16 | 3541 | 13253 | 90611637 |
| CD4 lymphocytes decreased | 36.06 | 19.26 | 9 | 3548 | 1538 | 90623352 |
| Plasma cell myeloma | 34.69 | 19.26 | 21 | 3536 | 40807 | 90584083 |
| Intussusception | 34.09 | 19.26 | 8 | 3549 | 1057 | 90623833 |
| Smooth muscle cell neoplasm | 32.07 | 19.26 | 8 | 3549 | 1365 | 90623525 |
| Diarrhoea | 24.06 | 19.26 | 86 | 3471 | 939104 | 89685786 |
| Chronic graft versus host disease | 23.35 | 19.26 | 8 | 3549 | 4131 | 90620759 |
| Herpes zoster | 22.70 | 19.26 | 23 | 3534 | 94621 | 90530269 |
| Necrotising retinitis | 22.26 | 19.26 | 5 | 3552 | 544 | 90624346 |
| Acute myeloid leukaemia | 21.17 | 19.26 | 12 | 3545 | 20628 | 90604262 |
| Pericardial drainage | 19.46 | 19.26 | 4 | 3553 | 286 | 90624604 |
| Post transplant lymphoproliferative disorder | 19.31 | 19.26 | 8 | 3549 | 6941 | 90617949 |
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 |
|---|---|---|---|---|---|---|
| Ureaplasma infection | 47.76 | 22.70 | 10 | 2080 | 626 | 42618619 |
| Febrile neutropenia | 42.95 | 22.70 | 49 | 2041 | 185654 | 42433591 |
| Herpes simplex pneumonia | 42.91 | 22.70 | 8 | 2082 | 274 | 42618971 |
| Gastrointestinal tract mucosal pigmentation | 37.17 | 22.70 | 8 | 2082 | 571 | 42618674 |
| Meralgia paraesthetica | 33.53 | 22.70 | 6 | 2084 | 163 | 42619082 |
| Tuberculosis liver | 31.88 | 22.70 | 5 | 2085 | 59 | 42619186 |
| Lip haemorrhage | 28.37 | 22.70 | 7 | 2083 | 913 | 42618332 |
| Hyperammonaemia | 22.96 | 22.70 | 10 | 2080 | 7856 | 42611389 |
FDA Adverse Event Reporting System (Geriatric)
| 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 |
|---|---|---|---|---|---|---|
| Aplastic anaemia | 58.52 | 17.99 | 26 | 4758 | 24282 | 110560233 |
| Febrile neutropenia | 45.54 | 17.99 | 62 | 4722 | 316705 | 110267810 |
| Herpes simplex pneumonia | 41.26 | 17.99 | 8 | 4776 | 385 | 110584130 |
| Ureaplasma infection | 40.15 | 17.99 | 10 | 4774 | 1536 | 110582979 |
| Herpes zoster | 32.32 | 17.99 | 31 | 4753 | 108348 | 110476167 |
| Gastrointestinal tract mucosal pigmentation | 31.87 | 17.99 | 8 | 4776 | 1269 | 110583246 |
| Tuberculosis liver | 30.07 | 17.99 | 5 | 4779 | 99 | 110584416 |
| CD4 lymphocytes decreased | 29.37 | 17.99 | 9 | 4775 | 2965 | 110581550 |
| Bacteraemia | 27.29 | 17.99 | 19 | 4765 | 42371 | 110542144 |
| Platelet count decreased | 27.05 | 17.99 | 41 | 4743 | 230402 | 110354113 |
| Lip haemorrhage | 26.06 | 17.99 | 7 | 4777 | 1445 | 110583070 |
| Plasma cell myeloma | 22.64 | 17.99 | 20 | 4764 | 62916 | 110521599 |
| Pathogen resistance | 21.82 | 17.99 | 12 | 4772 | 17660 | 110566855 |
| Meralgia paraesthetica | 21.19 | 17.99 | 5 | 4779 | 612 | 110583903 |
| Neuropathy peripheral | 21.17 | 17.99 | 32 | 4752 | 179245 | 110405270 |
| Necrotising retinitis | 20.86 | 17.99 | 6 | 4778 | 1590 | 110582925 |
| Drug resistance | 20.44 | 17.99 | 18 | 4766 | 56356 | 110528159 |
| White blood cell count decreased | 19.11 | 17.99 | 35 | 4749 | 229355 | 110355160 |
| Hyperammonaemia | 18.84 | 17.99 | 10 | 4774 | 13722 | 110570793 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J05AB09 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Nucleosides and nucleotides excl. reverse transcriptase inhibitors |
| ATC | S01AD07 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIINFECTIVES Antivirals |
| FDA MoA | N0000020060 | DNA Polymerase Inhibitors |
| FDA EXT | N0000175459 | Nucleoside Analog |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000998 | Antiviral Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D019384 | Nucleic Acid Synthesis Inhibitors |
| CHEBI has role | CHEBI:22587 | antiviral agent |
| CHEBI has role | CHEBI:35705 | immunosuppressive agent |
| CHEBI has role | CHEBI:36044 | antiviral drug |
| CHEBI has role | CHEBI:50266 | prodrug |
| CHEBI has role | CHEBI:64952 | anti-HSV agent |
| CHEBI has role | CHEBI:66981 | ophthalmology drug |
| FDA EPC | N0000180187 | Herpes Simplex Virus Nucleoside Analog DNA Polymerase Inhibitor |
Related Drugs by ATC class:
J05AB Nucleosides and nucleotides excl. reverse transcriptase inhibitors 11 drugs
S01AD Antivirals 6 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Herpes zoster | indication | 4740000 | DOID:8536 |
| Herpes simplex | indication | 88594005 | DOID:8566 |
| Recurrent herpes simplex labialis | indication | 402892009 | |
| Recurrent genital herpes simplex | indication | 402894005 | |
| Suppression of Recurrent Herpes Simplex Infection | indication | ||
| Recurrent Mucocutaneous Herpes Simplex in Human Immunodeficiency Virus Infected Patients | indication | ||
| Suppression of Recurrent Herpes Simplex Infection in HIV | off-label use | ||
| Prevention of Herpes Zoster in Immunocompromised Patient | off-label use | ||
| Kidney disease | contraindication | 90708001 | DOID:557 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.86 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| DNA polymerase catalytic subunit | Enzyme | INHIBITOR | WOMBAT-PK | CHEMBL | |||||
| DNA polymerase catalytic subunit | Enzyme | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4020882 | VUID |
| N0000148380 | NUI |
| D00317 | KEGG_DRUG |
| 4020882 | VANDF |
| C0209227 | UMLSCUI |
| CHEBI:4974 | CHEBI |
| CHEMBL880 | ChEMBL_ID |
| DB00426 | DRUGBANK_ID |
| D000077595 | MESH_DESCRIPTOR_UI |
| 3324 | PUBCHEM_CID |
| 11629 | IUPHAR_LIGAND_ID |
| 6438 | INN_ID |
| QIC03ANI02 | UNII |
| 151733 | RXNORM |
| 119086 | MMSL |
| 1730 | MMSL |
| 4712 | MMSL |
| d03775 | MMSL |
| 004470 | NDDF |
| 387557001 | SNOMEDCT_US |
| 96097002 | SNOMEDCT_US |
| QIC03ANI02 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Famciclovir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-8117 | TABLET, FILM COATED | 125 mg | ORAL | ANDA | 25 sections |
| Famciclovir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-8118 | TABLET, FILM COATED | 250 mg | ORAL | ANDA | 25 sections |
| Famciclovir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-8119 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 25 sections |
| Famciclovir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17856-0705 | TABLET, FILM COATED | 250 mg | ORAL | ANDA | 25 sections |
| Famciclovir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17856-0706 | TABLET, FILM COATED | 125 mg | ORAL | ANDA | 25 sections |
| Famciclovir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17856-0708 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 25 sections |
| Famciclovir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 31722-706 | TABLET, FILM COATED | 125 mg | ORAL | ANDA | 25 sections |
| Famciclovir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 31722-707 | TABLET, FILM COATED | 250 mg | ORAL | ANDA | 25 sections |
| Famciclovir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 31722-708 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 25 sections |
| Famciclovir | Human Prescription Drug Label | 1 | 33342-024 | TABLET, FILM COATED | 125 mg | ORAL | ANDA | 25 sections |
| Famciclovir | Human Prescription Drug Label | 1 | 33342-025 | TABLET, FILM COATED | 250 mg | ORAL | ANDA | 25 sections |
| Famciclovir | Human Prescription Drug Label | 1 | 33342-026 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 25 sections |
| Famciclovir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-414 | TABLET, FILM COATED | 125 mg | ORAL | ANDA | 25 sections |
| Famciclovir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-415 | TABLET, FILM COATED | 250 mg | ORAL | ANDA | 25 sections |
| Famciclovir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-416 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 25 sections |
| Famciclovir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 53002-0640 | TABLET, FILM COATED | 250 mg | ORAL | ANDA | 25 sections |
| Famciclovir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-5905 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 28 sections |
| Famciclovir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55289-168 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 25 sections |
| Famciclovir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55289-168 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 25 sections |
| FAMCICLOVIR | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60505-3245 | TABLET, FILM COATED | 125 mg | ORAL | ANDA | 23 sections |
| FAMCICLOVIR | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60505-3246 | TABLET, FILM COATED | 250 mg | ORAL | ANDA | 23 sections |
| FAMCICLOVIR | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60505-3247 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 23 sections |
| Famciclovir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63187-998 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 24 sections |
| Famciclovir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-7890 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 25 sections |
| Famciclovir | Human Prescription Drug Label | 1 | 64980-349 | TABLET, FILM COATED | 125 mg | ORAL | ANDA | 26 sections |
| Famciclovir | Human Prescription Drug Label | 1 | 64980-350 | TABLET, FILM COATED | 250 mg | ORAL | ANDA | 26 sections |
| Famciclovir | Human Prescription Drug Label | 1 | 64980-351 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 26 sections |
| Famciclovir | Human Prescription Drug Label | 1 | 65862-465 | TABLET, FILM COATED | 125 mg | ORAL | ANDA | 26 sections |
| Famciclovir | Human Prescription Drug Label | 1 | 65862-466 | TABLET, FILM COATED | 250 mg | ORAL | ANDA | 26 sections |
| Famciclovir | Human Prescription Drug Label | 1 | 65862-467 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 26 sections |