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Details

Stereochemistry ACHIRAL
Molecular Formula C18H24N4O
Molecular Weight 312.4094
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of GRANISETRON

SMILES

CN1N=C(C(=O)N[C@@H]2C[C@@H]3CCC[C@H](C2)N3C)C4=CC=CC=C14

InChI

InChIKey=MFWNKCLOYSRHCJ-BTTYYORXSA-N
InChI=1S/C18H24N4O/c1-21-13-6-5-7-14(21)11-12(10-13)19-18(23)17-15-8-3-4-9-16(15)22(2)20-17/h3-4,8-9,12-14H,5-7,10-11H2,1-2H3,(H,19,23)/t12-,13+,14-

HIDE SMILES / InChI
Molecular Formula C18H24N4O
Molecular Weight 312.4094
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 3 / 3
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022445s000lbl.pdf

Granisetron is a selective inhibitor of type 3 serotonergic (5-HT3) receptors. The drug is structurally and pharmacologically related to ondansetron, another selective inhibitor of 5-HT3 receptors. The serontonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery, and centrally in the chemoreceptor trigger zone of the area postrema. The temporal relationship between the emetogenic action of emetogenic drugs and the release of serotonin, as well as the efficacy of antiemetic agents suggest that chemotherapeutic agents release serotonin from the enterochromaffin cells of the small intestine by causing degenerative changes in the GI tract. The serotonin then stimulates the vagal and splanchnic nerve receptors that project to the medullary vomiting center, as well as the 5-HT3 receptors in the area postrema, thus initiating the vomiting reflex, causing nausea and vomiting. Granisetron is a potent, selective antagonist of 5-HT3 receptors. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone. Granisetron is used for the prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer therapy (including high dose cisplatin), postoperation, and radiation (including total body irradiation and daily fractionated abdominal radiation).

CNS Activity

CNS Penetrant
2554
Curator's Comment: The increasing brain/blood concentration ratio of granisetron suggests that granisetron penetrates the blood-brain barrier in rats.

Originator

Approval Year

1993
136
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2778
 1.45 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Secondary
Approved
8429
SUSTOL

Approved Use

SUSTOL is a serotonin-3 (5-HT3) receptor antagonist indicated in combination with other antiemetics in adults for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic chemotherapy (MEC) or anthracycline and cyclophosphamide (AC) combination chemotherapy regimens.

Launch Date

1992
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
4.948 ng/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/22452942
10 μg/kg bw single, intravenous
dose: 10 μg/kg bw
route of administration: Intravenous
experiment type: SINGLE
co-administered:
GRANISETRON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
36.87 ng × h/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/22452942
10 μg/kg bw single, intravenous
dose: 10 μg/kg bw
route of administration: Intravenous
experiment type: SINGLE
co-administered:
GRANISETRON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
5 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/22452942
10 μg/kg bw single, intravenous
dose: 10 μg/kg bw
route of administration: Intravenous
experiment type: SINGLE
co-administered:
GRANISETRON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
2 mg 2 times / day multiple, oral
Highest studied dose
Dose: 2 mg, 2 times / day
Route: oral
Route: multiple
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
unhealthy, 50.6 years (range: 23-76 years)
n = 233
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 50.6 years (range: 23-76 years)
Sex: M+F
Population Size: 233
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
Other AEs: Constipation, Headache...
Other AEs:
Constipation (27.5%)
Headache (17.6%)
Leukopenia (15%)
Asthenia (6.9%)
Abdominal pain (9%)
Decreased appetite (5.6%)
Anemia (1.3%)
Diarrhea (4.3%)
Abnormal liver function tests (2.6%)
Alopecia (3%)
Pain (0.4%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
160 ug/kg single, intravenous
Highest studied dose
Dose: 160 ug/kg
Route: intravenous
Route: single
Dose: 160 ug/kg
Co-administed with::
cisplatin(>50 mg/m^2)
Sources:
https://pubmed.ncbi.nlm.nih.gov/8032704/
unhealthy, 54
n = 165
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 54
Sex: M+F
Population Size: 165
Sources:
https://pubmed.ncbi.nlm.nih.gov/8032704/
Other AEs: Headache, Constipation...
Other AEs:
Headache (13.9%)
Constipation (4.2%)
Somnolence (2.4%)
Dizziness (1.2%)
Dyspepsia (1.8%)
Back pain (3%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/8032704/
15 mg single, subcutaneous
Highest studied dose
Dose: 15 mg
Route: subcutaneous
Route: single
Dose: 15 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
unhealthy, 64.3
n = 13
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 64.3
Sex: M+F
Population Size: 13
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
Other AEs: Constipation, Diarrhea...
Other AEs:
Constipation (23.1%)
Diarrhea (15.4%)
Headache (30.8%)
Fatigue (15.4%)
Anorexia (15.4%)
Weight loss (7.7%)
Dizziness (7.7%)
Neutropenia (15.4%)
Mucosal inflammation (15.4%)
Dyspnea (7.7%)
Insomnia (7.7%)
Thrombocytopenia (7.7%)
Injection site bruising (7.7%)
Pain injection site (2.2%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Other AEs: Pain, Constipation...
Other AEs:
Pain (10.1%)
Constipation (9.4%)
Anemia (9.4%)
Headache (8.6%)
Fever (7.9%)
Abdominal pain (6%)
Hepatic enzymes increased (5.6%)
Insomnia (4.9%)
Bradycardia (4.5%)
Dizziness (4.1%)
Leukocytosis (3.7%)
Anxiety (3.4%)
Hypotension (3.4%)
Diarrhea (3.4%)
Flatulence (3%)
Infection (3%)
Dyspepsia (3%)
Hypertension (2.6%)
Urinary tract infection (2.6%)
Oliguria (2.2%)
Coughing (2.2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
40 ug/kg single, intravenous
Recommended
Dose: 40 ug/kg
Route: intravenous
Route: single
Dose: 40 ug/kg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 1268
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Population Size: 1268
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Other AEs: Headache, Asthenia...
Other AEs:
Headache (14%)
Asthenia (5%)
Somnolence (4%)
Diarrhea (4%)
Constipation (3%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
AEs

AEs

AESignificanceDosePopulation
Pain 0.4%
2 mg 2 times / day multiple, oral
Highest studied dose
Dose: 2 mg, 2 times / day
Route: oral
Route: multiple
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
unhealthy, 50.6 years (range: 23-76 years)
n = 233
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 50.6 years (range: 23-76 years)
Sex: M+F
Population Size: 233
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
Anemia 1.3%
2 mg 2 times / day multiple, oral
Highest studied dose
Dose: 2 mg, 2 times / day
Route: oral
Route: multiple
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
unhealthy, 50.6 years (range: 23-76 years)
n = 233
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 50.6 years (range: 23-76 years)
Sex: M+F
Population Size: 233
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
Leukopenia 15%
2 mg 2 times / day multiple, oral
Highest studied dose
Dose: 2 mg, 2 times / day
Route: oral
Route: multiple
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
unhealthy, 50.6 years (range: 23-76 years)
n = 233
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 50.6 years (range: 23-76 years)
Sex: M+F
Population Size: 233
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
Headache 17.6%
2 mg 2 times / day multiple, oral
Highest studied dose
Dose: 2 mg, 2 times / day
Route: oral
Route: multiple
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
unhealthy, 50.6 years (range: 23-76 years)
n = 233
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 50.6 years (range: 23-76 years)
Sex: M+F
Population Size: 233
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
Abnormal liver function tests 2.6%
2 mg 2 times / day multiple, oral
Highest studied dose
Dose: 2 mg, 2 times / day
Route: oral
Route: multiple
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
unhealthy, 50.6 years (range: 23-76 years)
n = 233
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 50.6 years (range: 23-76 years)
Sex: M+F
Population Size: 233
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
Constipation 27.5%
2 mg 2 times / day multiple, oral
Highest studied dose
Dose: 2 mg, 2 times / day
Route: oral
Route: multiple
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
unhealthy, 50.6 years (range: 23-76 years)
n = 233
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 50.6 years (range: 23-76 years)
Sex: M+F
Population Size: 233
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
Alopecia 3%
2 mg 2 times / day multiple, oral
Highest studied dose
Dose: 2 mg, 2 times / day
Route: oral
Route: multiple
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
unhealthy, 50.6 years (range: 23-76 years)
n = 233
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 50.6 years (range: 23-76 years)
Sex: M+F
Population Size: 233
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
Diarrhea 4.3%
2 mg 2 times / day multiple, oral
Highest studied dose
Dose: 2 mg, 2 times / day
Route: oral
Route: multiple
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
unhealthy, 50.6 years (range: 23-76 years)
n = 233
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 50.6 years (range: 23-76 years)
Sex: M+F
Population Size: 233
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
Decreased appetite 5.6%
2 mg 2 times / day multiple, oral
Highest studied dose
Dose: 2 mg, 2 times / day
Route: oral
Route: multiple
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
unhealthy, 50.6 years (range: 23-76 years)
n = 233
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 50.6 years (range: 23-76 years)
Sex: M+F
Population Size: 233
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
Asthenia 6.9%
2 mg 2 times / day multiple, oral
Highest studied dose
Dose: 2 mg, 2 times / day
Route: oral
Route: multiple
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
unhealthy, 50.6 years (range: 23-76 years)
n = 233
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 50.6 years (range: 23-76 years)
Sex: M+F
Population Size: 233
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
Abdominal pain 9%
2 mg 2 times / day multiple, oral
Highest studied dose
Dose: 2 mg, 2 times / day
Route: oral
Route: multiple
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
unhealthy, 50.6 years (range: 23-76 years)
n = 233
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 50.6 years (range: 23-76 years)
Sex: M+F
Population Size: 233
Sources:
https://pubmed.ncbi.nlm.nih.gov/7758060/
Dizziness 1.2%
160 ug/kg single, intravenous
Highest studied dose
Dose: 160 ug/kg
Route: intravenous
Route: single
Dose: 160 ug/kg
Co-administed with::
cisplatin(>50 mg/m^2)
Sources:
https://pubmed.ncbi.nlm.nih.gov/8032704/
unhealthy, 54
n = 165
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 54
Sex: M+F
Population Size: 165
Sources:
https://pubmed.ncbi.nlm.nih.gov/8032704/
Dyspepsia 1.8%
160 ug/kg single, intravenous
Highest studied dose
Dose: 160 ug/kg
Route: intravenous
Route: single
Dose: 160 ug/kg
Co-administed with::
cisplatin(>50 mg/m^2)
Sources:
https://pubmed.ncbi.nlm.nih.gov/8032704/
unhealthy, 54
n = 165
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 54
Sex: M+F
Population Size: 165
Sources:
https://pubmed.ncbi.nlm.nih.gov/8032704/
Headache 13.9%
160 ug/kg single, intravenous
Highest studied dose
Dose: 160 ug/kg
Route: intravenous
Route: single
Dose: 160 ug/kg
Co-administed with::
cisplatin(>50 mg/m^2)
Sources:
https://pubmed.ncbi.nlm.nih.gov/8032704/
unhealthy, 54
n = 165
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 54
Sex: M+F
Population Size: 165
Sources:
https://pubmed.ncbi.nlm.nih.gov/8032704/
Somnolence 2.4%
160 ug/kg single, intravenous
Highest studied dose
Dose: 160 ug/kg
Route: intravenous
Route: single
Dose: 160 ug/kg
Co-administed with::
cisplatin(>50 mg/m^2)
Sources:
https://pubmed.ncbi.nlm.nih.gov/8032704/
unhealthy, 54
n = 165
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 54
Sex: M+F
Population Size: 165
Sources:
https://pubmed.ncbi.nlm.nih.gov/8032704/
Back pain 3%
160 ug/kg single, intravenous
Highest studied dose
Dose: 160 ug/kg
Route: intravenous
Route: single
Dose: 160 ug/kg
Co-administed with::
cisplatin(>50 mg/m^2)
Sources:
https://pubmed.ncbi.nlm.nih.gov/8032704/
unhealthy, 54
n = 165
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 54
Sex: M+F
Population Size: 165
Sources:
https://pubmed.ncbi.nlm.nih.gov/8032704/
Constipation 4.2%
160 ug/kg single, intravenous
Highest studied dose
Dose: 160 ug/kg
Route: intravenous
Route: single
Dose: 160 ug/kg
Co-administed with::
cisplatin(>50 mg/m^2)
Sources:
https://pubmed.ncbi.nlm.nih.gov/8032704/
unhealthy, 54
n = 165
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 54
Sex: M+F
Population Size: 165
Sources:
https://pubmed.ncbi.nlm.nih.gov/8032704/
Anorexia 15.4%
15 mg single, subcutaneous
Highest studied dose
Dose: 15 mg
Route: subcutaneous
Route: single
Dose: 15 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
unhealthy, 64.3
n = 13
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 64.3
Sex: M+F
Population Size: 13
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
Diarrhea 15.4%
15 mg single, subcutaneous
Highest studied dose
Dose: 15 mg
Route: subcutaneous
Route: single
Dose: 15 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
unhealthy, 64.3
n = 13
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 64.3
Sex: M+F
Population Size: 13
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
Fatigue 15.4%
15 mg single, subcutaneous
Highest studied dose
Dose: 15 mg
Route: subcutaneous
Route: single
Dose: 15 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
unhealthy, 64.3
n = 13
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 64.3
Sex: M+F
Population Size: 13
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
Mucosal inflammation 15.4%
15 mg single, subcutaneous
Highest studied dose
Dose: 15 mg
Route: subcutaneous
Route: single
Dose: 15 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
unhealthy, 64.3
n = 13
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 64.3
Sex: M+F
Population Size: 13
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
Neutropenia 15.4%
15 mg single, subcutaneous
Highest studied dose
Dose: 15 mg
Route: subcutaneous
Route: single
Dose: 15 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
unhealthy, 64.3
n = 13
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 64.3
Sex: M+F
Population Size: 13
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
Pain injection site 2.2%
15 mg single, subcutaneous
Highest studied dose
Dose: 15 mg
Route: subcutaneous
Route: single
Dose: 15 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
unhealthy, 64.3
n = 13
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 64.3
Sex: M+F
Population Size: 13
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
Constipation 23.1%
15 mg single, subcutaneous
Highest studied dose
Dose: 15 mg
Route: subcutaneous
Route: single
Dose: 15 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
unhealthy, 64.3
n = 13
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 64.3
Sex: M+F
Population Size: 13
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
Headache 30.8%
15 mg single, subcutaneous
Highest studied dose
Dose: 15 mg
Route: subcutaneous
Route: single
Dose: 15 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
unhealthy, 64.3
n = 13
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 64.3
Sex: M+F
Population Size: 13
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
Dizziness 7.7%
15 mg single, subcutaneous
Highest studied dose
Dose: 15 mg
Route: subcutaneous
Route: single
Dose: 15 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
unhealthy, 64.3
n = 13
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 64.3
Sex: M+F
Population Size: 13
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
Dyspnea 7.7%
15 mg single, subcutaneous
Highest studied dose
Dose: 15 mg
Route: subcutaneous
Route: single
Dose: 15 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
unhealthy, 64.3
n = 13
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 64.3
Sex: M+F
Population Size: 13
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
Injection site bruising 7.7%
15 mg single, subcutaneous
Highest studied dose
Dose: 15 mg
Route: subcutaneous
Route: single
Dose: 15 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
unhealthy, 64.3
n = 13
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 64.3
Sex: M+F
Population Size: 13
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
Insomnia 7.7%
15 mg single, subcutaneous
Highest studied dose
Dose: 15 mg
Route: subcutaneous
Route: single
Dose: 15 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
unhealthy, 64.3
n = 13
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 64.3
Sex: M+F
Population Size: 13
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
Thrombocytopenia 7.7%
15 mg single, subcutaneous
Highest studied dose
Dose: 15 mg
Route: subcutaneous
Route: single
Dose: 15 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
unhealthy, 64.3
n = 13
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 64.3
Sex: M+F
Population Size: 13
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
Weight loss 7.7%
15 mg single, subcutaneous
Highest studied dose
Dose: 15 mg
Route: subcutaneous
Route: single
Dose: 15 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
unhealthy, 64.3
n = 13
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Age Group: 64.3
Sex: M+F
Population Size: 13
Sources:
https://pubmed.ncbi.nlm.nih.gov/25834466/
Pain 10.1%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Coughing 2.2%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Oliguria 2.2%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Hypertension 2.6%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Urinary tract infection 2.6%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Dyspepsia 3%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Flatulence 3%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Infection 3%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Anxiety 3.4%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Diarrhea 3.4%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Hypotension 3.4%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Leukocytosis 3.7%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Dizziness 4.1%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Bradycardia 4.5%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Insomnia 4.9%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Hepatic enzymes increased 5.6%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Abdominal pain 6%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Fever 7.9%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Headache 8.6%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Anemia 9.4%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Constipation 9.4%
1 mg single, intravenous
Recommended
Dose: 1 mg
Route: intravenous
Route: single
Dose: 1 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Headache 14%
40 ug/kg single, intravenous
Recommended
Dose: 40 ug/kg
Route: intravenous
Route: single
Dose: 40 ug/kg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 1268
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Population Size: 1268
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Constipation 3%
40 ug/kg single, intravenous
Recommended
Dose: 40 ug/kg
Route: intravenous
Route: single
Dose: 40 ug/kg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 1268
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Population Size: 1268
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Diarrhea 4%
40 ug/kg single, intravenous
Recommended
Dose: 40 ug/kg
Route: intravenous
Route: single
Dose: 40 ug/kg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 1268
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Population Size: 1268
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Somnolence 4%
40 ug/kg single, intravenous
Recommended
Dose: 40 ug/kg
Route: intravenous
Route: single
Dose: 40 ug/kg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 1268
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Population Size: 1268
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Asthenia 5%
40 ug/kg single, intravenous
Recommended
Dose: 40 ug/kg
Route: intravenous
Route: single
Dose: 40 ug/kg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
unhealthy
n = 1268
Health Status: unhealthy
Condition: nausea and vomiting, chemotherapy-Induced
Population Size: 1268
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020239s021,020305s014,021238s007lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1737
substrate
1037
substrate
1217
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A1
349

CYP1A2
1054

CYP1B1
92

CYP2A6
543

CYP2B6
664

CYP2C8
693

CYP2C18
138

CYP2C19
991

CYP2E1
667

CYP2J2
56

CYP3A5
395

CYP3A7
110
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1054
 likely
CYP1B1
92
 likely
CYP2B6
664
 likely
CYP2C19
991
 likely
CYP2C8
693
 likely
CYP2D6
1217
 likely
CYP2J2
56
 likely
CYP3A5
395
 likely
CYP3A7
110
 likely
CYP1A1
349
 major
unknown (co-administration study)
Comment: Administration of intravenous granisetron hydrochloride with phenobarbital, an enzyme inducer, resulted in a 25% increase in total plasma clearance of granisetron. The clinical significance of this interaction is not known.
Page: 113.0
CYP3A4
1737
 minor
unknown (co-administration study)
Comment: the potential for an in vivo pharmacokinetic interaction with ketoconazole is not known; Administration of intravenous granisetron hydrochloride with phenobarbital, an enzyme inducer, resulted in a 25% increase in total plasma clearance of granisetron. The clinical significance of this interaction is not known.
Page: 113.0
CYP2A6
543
 no
CYP2C18
138
 no
CYP2C9
1037
 no
CYP2E1
667
 no
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:5537
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:5537
ChemicalBook
CB2728852
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB2728852
ZINC
ZINC000100018854
http://zinc15.docking.org/substances/ZINC000100018854
eMolecules
32452667
https://www.emolecules.com/cgi-bin/more?vid=32452667
PubMed

PubMed

TitleDatePubMed
Effects of lerisetron, a new 5-HT3 receptor antagonist, on ipecacuanha-induced emesis in healthy volunteers.
2002
Effects of ondansetron, granisetron, ramosetron, and azasetron on human neutrophil functions.
2002
Sensitization of enteric reflexes in the rat colon in vitro.
2002 Apr 18
5-Hydroxytryptamine receptors, especially the 5-HT4 receptor, in guinea pig urinary bladder.
2002 Aug
Ondansetron but not granisetron affect cell volume regulation and potassium ion transport of glioma cells treated with estramustine phosphate.
2002 Aug
Progress in preventing chemotherapy-induced nausea and vomiting.
2002 Aug
Impaired gastrocolonic response and peristaltic reflex in slow-transit constipation: role of 5-HT(3) pathways.
2002 Aug
A 'modified de Gramont' regimen of fluorouracil, alone and with oxaliplatin, for advanced colorectal cancer.
2002 Aug 12
Triplet chemotherapy with vinorelbine, gemcitabine, and cisplatin for advanced non-small cell lung cancer: a phase II study.
2002 Dec 2
Ramosetron, a 5-HT3 receptor antagonist for the control of nausea and vomiting.
2002 Feb
Antiemetic effects of granisetron, droperidol and dexamethasone in otologic surgery.
2002 Jul
Irinotecan pharmacokinetics-pharmacodynamics: the clinical relevance of prolonged exposure to SN-38.
2002 Jul 15
Laxative and anti-diarrheal activity of polycarbophil in mice and rats.
2002 Jun
Involvement of serotonin and nitric oxide in endotoxin-induced gastric motility changes in conscious rats.
2002 Jun
ATP and 5-HT are the principal neurotransmitters in the descending excitatory reflex pathway of the guinea-pig ileum.
2002 Jun
Effectiveness of serotonin-receptor antagonist antiemetic therapy over successive courses of carboplatin-based chemotherapy.
2002 Jun
Identification of critical residues in loop E in the 5-HT3ASR binding site.
2002 Jun 13
Functional group interactions of a 5-HT3R antagonist.
2002 Jun 13
ATP as a putative sensory mediator: activation of intrinsic sensory neurons of the myenteric plexus via P2X receptors.
2002 Jun 15
Preoperative oral granisetron for the prevention of vomiting following paediatric surgery.
2002 Mar
Gateways to clinical trials.
2002 May
Comparison of granisetron and ramosetron for the prevention of nausea and vomiting after thyroidectomy.
2002 May
Granisetron vs ondansetron: is it a question of duration of 5-HT3 receptor blockade?
2002 May 20
A phase I trial of weekly gemcitabine and concurrent radiotherapy in patients with locally advanced pancreatic cancer.
2002 May 20
A dose-finding study of carboplatin-epirubicin-docetaxel in advanced epithelial ovarian cancer.
2002 May 6
Ramosetron for the prevention of cisplatin-induced acute emesis: a prospective randomized comparison with granisetron.
2002 May-Jun
Comparative study of low-dose oral granisetron plus dexamethasone and high-dose metoclopramide plus dexamethasone in prevention of nausea and vomiting induced by CHOP-therapy in young patients with non-Hodgkin's lymphoma.
2002 Nov
Oral granisetron revisited.
2002 Nov
Motilin regulates interdigestive gastric blood flow in dogs.
2002 Nov
The effect of serotonin and serotonin receptor antagonists on motion sickness in Suncus murinus.
2002 Nov
Phase I study of docetaxel in combination with cyclophosphamide as first-line chemotherapy for metastatic breast cancer.
2002 Nov 4
Compatibility and stability of 5-HT3 receptor antagonists: a pharmacology review.
2002 Nov-Dec
Prophylactic antiemetic efficacy of granisetron or ramosetron in patients undergoing thyroidectomy.
2002 Oct
Irinotecan, cisplatin and mitomycin in inoperable gastro-oesophageal and pancreatic cancers - a new active regimen.
2002 Oct 7
[Nausea disintegrating buccal tablet in the prevention of gastrointestinal reaction induced by anticancer drugs].
2002 Sep
In vivo assessment of acceleration of motor activity associated with acetylcholine release via 5-hydroxytryptamine4 receptor in dog intestine.
2002 Sep
Comparison of granisetron with granisetron plus droperidol combination prophylaxis in post-operative nausea and vomiting after laparoscopic cholecystectomy.
2002 Sep-Oct
Treatment of vomiting after paediatric strabismus surgery with granisetron, droperidol, and metoclopramide.
2002 Sep-Oct
5-HT3-receptor antagonists and the cytochrome P450 system: clinical implications.
2002 Sep-Oct
Analysis of purinergic and cholinergic fast synaptic transmission to identified myenteric neurons.
2003
Combination therapy with granisetron, methylprednisolone and droperidol as an antiemetic prophylaxis in CDDP-induced delayed emesis for gynecologic cancer.
2003
Severe pruritus in a haemodialysed patient: dramatic improvement with granisetron.
2003 Feb
Effects on muscle pain by intramuscular injection of granisetron in patients with fibromyalgia.
2003 Feb
A randomized double-blind trial to compare the clinical efficacy of granisetron with metoclopramide, both combined with dexamethasone in the prophylaxis of chemotherapy-induced delayed emesis.
2003 Feb
Granisetron: relating pharmacology to clinical efficacy.
2003 Feb
Survival with dacarbazine and fotemustine in newly diagnosed glioblastoma multiforme.
2003 Feb 24
Granisetron plus dexamethasone versus granisetron alone in the prevention of vomiting induced by conditioning for stem cell transplantation: a prospective randomized study.
2003 Jan
Comparison of granisetron and granisetron plus dexamethasone for the prevention of postoperative nausea and vomiting after laparoscopic cholecystectomy.
2003 Jan
Feasibility of combination chemotherapy with cisplatin and etoposide for haemodialysis patients with lung cancer.
2003 Jan 13
Pharmacological characterization of the 5-HT1A, 5-HT2 and 5-HT3 receptors in the bovine ciliary muscle.
2003 Mar 7
Patents

Patents

JP2004513061A
11
JP2006516976A
30

Sample Use Guides

In Vivo Use Guide
IV: 10 mcg/kg over 5 minutes, beginning 30 minutes before initiation of chemotherapy. Orally: 2 mg, given up to 1 hour before chemotherapy, or 1 mg twice a day (the first dose is given up to 1 hour before chemotherapy, and the second dose is given 12 hours later). Granisetron transdermal system: Apply a single patch to the upper outer arm a minimum of 24 hours before chemotherapy. The patch may be applied up to a maximum of 48 hours before chemotherapy as appropriate. Remove the patch a minimum of 24 hours after completion of chemotherapy. The patch can be worn for up to 7 days depending on the duration of the chemotherapy regimen. Granisetron transdermal system is a 52 cm2 patch containing 34.3 mg of granisetron. The patch releases 3.1 mg of granisetron per 24 hours for up to 7 days.
Route of Administration: Other
In Vitro Use Guide
Granisetron (1 uM) shifted the response curves to mucosally applied 5-HT to the right in a parallel and surmountable manner in the guinea pig isolated ileum.
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:55:10 GMT 2023
Edited
by admin
on Fri Dec 15 15:55:10 GMT 2023
Record UNII
WZG3J2MCOL
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
GRANISETRON
INN   JAN   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
GRANISETRON [USAN]
Common Name English
GRANISETRON [JAN]
Common Name English
APF530
Code English
LY-278584
Code English
GRANISETRON [VANDF]
Common Name English
GRANISETRON [USP MONOGRAPH]
Common Name English
GRANISETRON [USP-RS]
Common Name English
APF-530
Code English
Granisetron [WHO-DD]
Common Name English
1H-INDAZOLE-3-CARBOXAMIDE, 1-METHYL-N-(9-METHYL-9-AZABICYCLO(3.3.1)NON-3-YL)-, ENDO-
Common Name English
GRANISETRON [MI]
Common Name English
BRL-43694
Code English
GRANISETRON [ORANGE BOOK]
Common Name English
BRL 43694
Code English
granisetron [INN]
Common Name English
SANCUSO
Brand Name English
1-Methyl-N-(9-methyl-endo-9-azabicyclo[3.3.1]non-3-yl)-1H-indazole-3-carboxamide
Common Name English
SUSTOL
Brand Name English
Classification Tree Code System Code
NCI_THESAURUS C94726
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
NCI_THESAURUS C267
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
NDF-RT N0000175817
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
WHO-VATC QA04AA02
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
LIVERTOX 467
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
WHO-ATC A04AA02
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
NDF-RT N0000175818
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
EMA ASSESSMENT REPORTS SANCUSO (AUTHORIZED: VOMITTING)
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
Code System Code Type Description
INN
6230
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
DRUG BANK
DB00889
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
MERCK INDEX
m5842
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY Merck Index
CAS
109889-09-0
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
EPA CompTox
DTXSID0023111
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
DAILYMED
WZG3J2MCOL
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
ChEMBL
CHEMBL289469
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
USAN
DD-30
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
IUPHAR
2300
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
SMS_ID
100000084258
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
MESH
D017829
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
NCI_THESAURUS
C62031
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
CAS
124998-65-8
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
NON-SPECIFIC STEREOCHEMISTRY
WIKIPEDIA
GRANISETRON
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
FDA UNII
WZG3J2MCOL
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
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RS_ITEM_NUM
1298092
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
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EVMPD
SUB07964MIG
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
CHEBI
5537
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
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DRUG CENTRAL
1329
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
RXCUI
26237
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY RxNorm
Related Record Type Details
Structure of GRANISETRON HYDROCHLORIDE
SALT/SOLVATE -> PARENT
Structure of GRANISETRON H-3
LABELED -> NON-LABELED
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
Structure of GRANISETRON
EXCRETED UNCHANGED
Based on a study with intravenous injection, approximately 12% of the dose is excreted unchanged in the urine of healthy subjects in 48 hours.
AMOUNT EXCRETED
URINE
5-HYDROXYTRYPTAMINE RECEPTOR 3A
TARGET -> INHIBITOR
IC50
Related Record Type Details
Structure of 7-HYDROXYGRANISETRON
METABOLITE ACTIVE -> PARENT
After both oral and intravenous administration, the metabolite is present at about 10% of that of the parent (Clarke et al., 1994; Boppana, 1995). Assuming similar free fractions, it can be estimated that the metabolite would contribute about 20% of the activity of the parent.
Related Record Type Details
Structure of 3-CARBOXY-1-METHYLINDAZOLE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of 1-DESMETHYL GRANISETRON
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of 9-DESMETHYL GRANISETRON
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of 2-METHYL-N-(9-METHYL-9-AZABICYCLO(3.3.1)NON-3-YL)-,2H-INDAZOLE-3-CARBOXAMIDE, ENDO-
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Related Record Type Details
Structure of GRANISETRON
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC following patch application

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