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  1. pharmadog
  2. ›drugs
  3. ›SUSTOL
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SUSTOL

updated 3mo ago
by $HRTX HERON THERAPEUTICS, INC. /DE/🔗 ChEMBL
community read0 votes

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  • druggranisetron ER12 co-mentions · 3 sources
  • tagApproval12 co-mentions · 3 sources

Small molecule drug with a maximum clinical stage of Approval (across all indications), with 5 approved and 6 investigational indications.

targets

5-hydroxytryptamine receptor 3A

all catalysts(0)

nothing on the calendar yet

Trials studying SUSTOL

  • phase1Staccato® Granisetron Single Dose PKcompletedn=36
  • phase4Oral Akynzeo® vs Standard of Care in Preventing CINV in High-risk MEC Patients (MyRisk)completedn=414
  • phase1Granisetron 1 mg Tablets, Non-fastingcompletedn=80
  • phase1Granisetron 1 mg Tablets Under Fasting Conditionscompletedn=40
  • phase1Safety and Pharmacokinetics of Sancuso and IV Granisetron in Patients Aged 2 to 5 Yearswithdrawn
  • phase1Pharmacokinetics and Safety of Sancuso and IV Granisetron in Pediatrics Aged 6 to 12 Yearswithdrawn
  • phase1An Investigation on the Effect of Age and BMI on the Pharmacokinetics of Transdermal Granisetroncompletedn=60
  • phase1Safety and Pharmacokinetics of Sancuso and IV Granisetron in Patients Aged 13 to 17 Yearscompletedn=19
more trials →

News(0)

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brand
SUSTOL
trade names
Sancuso, Sustol
generic
GRANISETRON
MOA
12.1 Mechanism of Action Granisetron is a selective 5-hydroxytryptamine 3 (5-HT 3 ) receptor antagonist with little or no affinity for other serotonin receptors, including 5-HT 1 , 5-HT 1A , 5-HT 1B/C , 5-HT 2 ; for alpha 1- , alpha 2- , or beta-adrenoreceptors; for dopamine-D 2 ; or for histamine-H 1 ; benzodiazepine; picrotoxin or opioid receptors. Serotonin receptors of the 5-HT 3 type are located peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone of the area postrema. During chemotherapy that induces vomiting, mucosal enterochromaffin cells release serotonin, which stimulates 5-HT 3 receptors. This evokes vagal afferent discharge, inducing vomiting. Animal studies demonstrate that, in binding to 5-HT 3 receptors, granisetron blocks serotonin stimulation and subsequent vomiting after emetogenic stimuli such as cisplatin. In the ferret animal model, a single granisetron injection prevented vomiting due to high-dose cisplatin or arrested vomiting within 5 to 30 seconds.
indication
1 INDICATIONS AND USAGE SUSTOL is 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. SUSTOL is a serotonin-3 (5-HT 3 ) 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. ( 1 )
Data sources
ClinicalTrials.gov · OpenTargets
last refreshed 7m ago
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