granisetron Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| serotonin receptor antagonists (5-HT3) | 1329 | 109889-09-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 2 | mg | O |
| 3 | mg | P |
| 3.10 | mg | TD |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 100 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 11 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.03 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 60 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 3.70 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 9.10 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.35 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 5.20 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 29, 1993 | FDA | ROCHE |
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 |
|---|---|---|---|---|---|---|
| Tooth erosion | 98.08 | 48.29 | 13 | 292 | 132 | 2357648 |
| Dyspnoea | 94.48 | 48.29 | 39 | 266 | 78694 | 2279086 |
| Pulpitis dental | 87.50 | 48.29 | 12 | 293 | 160 | 2357620 |
| Vomiting | 84.10 | 48.29 | 35 | 270 | 71567 | 2286213 |
| Respiratory depth decreased | 82.36 | 48.29 | 9 | 296 | 11 | 2357769 |
| Nausea | 81.19 | 48.29 | 39 | 266 | 112150 | 2245630 |
| Periodontitis | 78.11 | 48.29 | 13 | 292 | 661 | 2357119 |
| Venous thrombosis limb | 60.58 | 48.29 | 10 | 295 | 481 | 2357299 |
| Serotonin syndrome | 56.60 | 48.29 | 13 | 292 | 3527 | 2354253 |
| Mucosal inflammation | 56.59 | 48.29 | 14 | 291 | 5210 | 2352570 |
| General physical health deterioration | 55.31 | 48.29 | 17 | 288 | 14122 | 2343658 |
| Sensory disturbance | 54.81 | 48.29 | 12 | 293 | 2620 | 2355160 |
| Chest discomfort | 54.77 | 48.29 | 17 | 288 | 14578 | 2343202 |
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 |
|---|---|---|---|---|---|---|
| Diarrhoea | 49.35 | 37.62 | 21 | 136 | 53831 | 1692793 |
| Colitis ischaemic | 43.31 | 37.62 | 8 | 149 | 880 | 1745744 |
| Vomiting | 38.40 | 37.62 | 16 | 141 | 38299 | 1708325 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A04AA02 | ALIMENTARY TRACT AND METABOLISM ANTIEMETICS AND ANTINAUSEANTS ANTIEMETICS AND ANTINAUSEANTS Serotonin (5HT3) antagonists |
| FDA MoA | N0000175817 | Serotonin 3 Receptor Antagonists |
| FDA EPC | N0000175818 | Serotonin-3 Receptor Antagonist |
| CHEBI has role | CHEBI:48279 | serotonergic antagonist |
| CHEBI has role | CHEBI:50919 | antiemetic |
| MeSH PA | D000932 | Antiemetics |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D005765 | Gastrointestinal Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018490 | Serotonin Agents |
| MeSH PA | D012702 | Serotonin Antagonists |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Chemotherapy-induced nausea and vomiting | indication | 236084000 | |
| Prevention of Radiation-Induced Nausea and Vomiting | indication | ||
| Prevention of Post-Operative Nausea and Vomiting | indication | ||
| Post-Operative Nausea and Vomiting | indication | ||
| Prolonged-Severe Nausea and Vomiting | off-label use | ||
| Hypokalemia | contraindication | 43339004 | |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Prolonged QT interval | contraindication | 111975006 | |
| Hypomagnesemia | contraindication | 190855004 | |
| Congenital long QT syndrome | contraindication | 442917000 | |
| Doxorubicin Induced Cardiomyopathy | contraindication |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.79 | acidic |
| pKa2 | 9.5 | 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 10MG/0.4ML (10MG/0.4ML) | SUSTOL | HERON THERAPS INC | N022445 | Aug. 9, 2016 | RX | INJECTION, EXTENDED RELEASE | SUBCUTANEOUS | 10357570 | Sept. 28, 2024 | PROPHYLACTIC TREATMENT OF NAUSEA AND VOMITING, INCLUDING PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED CHEMOTHERAPY |
| 10MG/0.4ML (10MG/0.4ML) | SUSTOL | HERON THERAPS INC | N022445 | Aug. 9, 2016 | RX | INJECTION, EXTENDED RELEASE | SUBCUTANEOUS | 8252305 | Sept. 28, 2024 | TREATMENT OR PREVENTION OF NAUSEA AND VOMITING |
| 10MG/0.4ML (10MG/0.4ML) | SUSTOL | HERON THERAPS INC | N022445 | Aug. 9, 2016 | RX | INJECTION, EXTENDED RELEASE | SUBCUTANEOUS | 9913910 | Sept. 28, 2024 | PROPHYLACTIC TREATMENT OF NAUSEA AND VOMITING, INCLUDING PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED CHEMOTHERAPY |
| 3.1MG/24HR | SANCUSO | KYOWA KIRIN | N022198 | Sept. 12, 2008 | RX | FILM, EXTENDED RELEASE | TRANSDERMAL | 7608282 | Jan. 22, 2025 | USE OF GRANISETRON TRANSDERMAL SYSTEM TO TREAT/PREVENT CHEMOTHERAPY INDUCED NAUSEA AND VOMITING |
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 |
|---|---|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 3A | Ion channel | ANTAGONIST | Ki | 8.70 | WOMBAT-PK | CHEMBL | |||
| Neuronal acetylcholine receptor; alpha4/beta2 | Ion channel | Ki | 4.42 | CHEMBL | |||||
| Solute carrier family 22 member 2 | Transporter | IC50 | 5.37 | CHEMBL | |||||
| Neuronal acetylcholine receptor subunit alpha-3 | Ion channel | Ki | 4.17 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 3B | Ion channel | Ki | 8.80 | CHEMBL | |||||
| Multidrug and toxin extrusion protein 1 | Transporter | IC50 | 5.30 | CHEMBL | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 5.43 | WOMBAT-PK | |||||
| Serotonin 3 (5-HT3) receptor | Ion channel | Ki | 9.46 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4020855 | VUID |
| N0000179527 | NUI |
| C0543476 | UMLSCUI |
| D00677 | KEGG_DRUG |
| 318F6L70J8 | UNII |
| 107007-99-8 | SECONDARY_CAS_RN |
| 108424001 | SNOMEDCT_US |
| 4023910 | VANDF |
| 25895 | MMSL |
| 003975 | NDDF |
| 26237 | RXNORM |
| 372489005 | SNOMEDCT_US |
| d03171 | MMSL |
| CHEMBL289469 | ChEMBL_ID |
| DB00889 | DRUGBANK_ID |
| CWB | PDB_CHEM_ID |
| CHEBI:5537 | CHEBI |
| 6230 | INN_ID |
| 5284566 | PUBCHEM_CID |
| CHEMBL1237080 | ChEMBL_ID |
| D017829 | MESH_DESCRIPTOR_UI |
| 2300 | IUPHAR_LIGAND_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Granisetron Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0143 | TABLET | 1 mg | ORAL | ANDA | 13 sections |
| Granisetron Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9744 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 17 sections |
| Granisetron Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9745 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 17 sections |
| Granisetron Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-221 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 13 sections |
| Granisetron Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-546 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 17 sections |
| Granisetron Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-547 | INJECTION | 0.10 mg | INTRAVENOUS | ANDA | 17 sections |
| Granisetron Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42043-390 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 13 sections |
| Sancuso | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42747-726 | PATCH | 3.10 mg | TRANSDERMAL | NDA | 18 sections |
| SUSTOL | HUMAN PRESCRIPTION DRUG LABEL | 1 | 47426-101 | INJECTION | 10 mg | SUBCUTANEOUS | NDA | 18 sections |
| Granisetron Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51991-735 | TABLET | 1 mg | ORAL | ANDA | 12 sections |
| Sancuso | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-5985 | PATCH | 3.10 mg | TRANSDERMAL | NDA | 17 sections |
| Granisetron Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55150-175 | INJECTION, SOLUTION | 1 mg | INTRAVENOUS | ANDA | 16 sections |
| Granisetron Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55150-176 | INJECTION, SOLUTION | 4 mg | INTRAVENOUS | ANDA | 16 sections |
| GRANISETRON HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55648-661 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 15 sections |
| GRANISETRON HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55648-662 | INJECTION | 0.10 mg | INTRAVENOUS | ANDA | 15 sections |
| Granisetron | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-317 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 16 sections |
| Granisetron | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-318 | INJECTION, SOLUTION | 1 mg | INTRAVENOUS | ANDA | 16 sections |
| Granisetron | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-319 | INJECTION, SOLUTION | 1 mg | INTRAVENOUS | ANDA | 16 sections |
| Granisetron hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63850-0005 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 13 sections |
| GRANISETRON HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64679-661 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 17 sections |
| GRANISETRON HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64679-662 | INJECTION | 0.10 mg | INTRAVENOUS | ANDA | 17 sections |
| GRANISETRON HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64679-841 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 17 sections |
| Granisetron | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66758-035 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 17 sections |
| Granisetron | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66758-036 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 17 sections |
| Granisetron Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67457-861 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 16 sections |
| Granisetron Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67457-863 | INJECTION, SOLUTION | 1 mg | INTRAVENOUS | ANDA | 16 sections |
| Granisetron Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67457-864 | INJECTION, SOLUTION | 1 mg | INTRAVENOUS | ANDA | 16 sections |
| Granisetron Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67877-184 | TABLET | 1 mg | ORAL | ANDA | 11 sections |
| GRANISETRON HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69097-195 | INJECTION | 0.10 mg | INTRAVENOUS | ANDA | 17 sections |
| GRANISETRON HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69097-197 | INJECTION | 4 mg | INTRAVENOUS | ANDA | 17 sections |