Granisetron

Summary

Granisetron (CHEMBL289469) is an approved small molecule (ATC A04AA02); indicated across 15 conditions including neoplasm and cervical carcinoma.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A04AA02
• Indications: 15 conditions
• Clinical trials: 81
• Chemistry: 312.4 Da · C18H24N4O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL289469
Name	Granisetron
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	3510
ATC	A04AA02
Molecular formula	C18H24N4O
Molecular weight	312.4
InChIKey	MFWNKCLOYSRHCJ-UHFFFAOYSA-N

SMILES: CN1C2CCCC1CC(C2)NC(=O)C3=NN(C4=CC=CC=C43)C

IUPAC name: 1-methyl-N-(9-methyl-9-azabicyclo[3.3.1]nonan-3-yl)indazole-3-carboxamide

Also known as: APF-530, APF530, BRL 43694, BRL-43694, Granisetron, LY-278584, Sancuso, Sustol, granisetron, SID90340785, GRANISETRON, [3H]-Granisetron

Parent form; salt/anhydrous children: CHEMBL1237080

Patent coverage: 194 distinct patent families (431 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 267 (62%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
	5-HT3A	Antagonist	8.8

Broader ChEMBL bioactivity targets: 11 (assay-derived). Sample: Solute carrier family 22 member 2, Multidrug and toxin extrusion protein 1, 5-hydroxytryptamine receptor 3A, Neuronal acetylcholine receptor; alpha4/beta2, Serotonin 3 (5-HT3) receptor, Serotonin 3 (5-HT3) receptor, Serotonin 3 (5-HT3) receptor, Voltage-gated inwardly rectifying potassium channel KCNH2, Neuronal acetylcholine receptor subunit alpha-3, 5-hydroxytryptamine receptor 3A.

Bioactivity

ChEMBL activities: 67 potent at pChembl ≥ 5 of 70 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
HTR3E	10.7	Kd	0.02	nM	CHEMBL_ACT_777273
P35563	10.6	Kd	0.03	nM	CHEMBL_ACT_887292
HTR3E	10.1	Kd	0.08	nM	CHEMBL_ACT_925216
HTR3E	9.9	Kd	0.13	nM	CHEMBL_ACT_777272
HTR3E	9.9	Kd	0.13	nM	CHEMBL_ACT_925215
HTR3B	9.8	Kd	0.16	nM	CHEMBL_ACT_13843615
HTR3A	9.72	Kd	0.19	nM	CHEMBL_ACT_13843625
HTR3B	9.7	Kd	0.2	nM	CHEMBL_ACT_13843617
HTR3B	9.7	Kd	0.2	nM	CHEMBL_ACT_13843621
HTR3B	9.66	Kd	0.22	nM	CHEMBL_ACT_13843620
HTR3B	9.6	Kd	0.25	nM	CHEMBL_ACT_13843619
P35563	9.6	Ki	0.25	nM	CHEMBL_ACT_766689
P35563	9.46	Ki	0.35	nM	CHEMBL_ACT_1016353
P35563	9.46	Ki	0.35	nM	CHEMBL_ACT_1019470
P35563	9.46	Ki	0.35	nM	CHEMBL_ACT_1508793
P35563	9.46	Ki	0.35	nM	CHEMBL_ACT_732756
HTR3A	9.44	Kd	0.36	nM	CHEMBL_ACT_13843626
HTR3A	9.43	Kd	0.37	nM	CHEMBL_ACT_13843624
HTR3A	9.39	Kd	0.41	nM	CHEMBL_ACT_13843630
HTR3A	9.36	Kd	0.44	nM	CHEMBL_ACT_13843623
HTR3A	9.31	Kd	0.49	nM	CHEMBL_ACT_13843627
P35563	9.3	Ki	0.5	nM	CHEMBL_ACT_1108847
HTR3A	9.28	Kd	0.53	nM	CHEMBL_ACT_13843633
P35563	9.23	Ki	0.59	nM	CHEMBL_ACT_777276
P35563	9.23	Ki	0.59	nM	CHEMBL_ACT_887293
HTR3A	9.22	Kd	0.6	nM	CHEMBL_ACT_13843632
P35563	9.22	Ki	0.6	nM	CHEMBL_ACT_651833
HTR3B	9.11	Kd	0.78	nM	CHEMBL_ACT_13843618
HTR3A	9.11	Kd	0.78	nM	CHEMBL_ACT_13843628
P35563	9.11	Ki	0.78	nM	CHEMBL_ACT_779197

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

15 indications (7 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
neoplasm	4	MONDO:0005070	EFO:0000616
cervical carcinoma	3	MONDO:0005131	EFO:0001061
hepatocellular carcinoma	3	MONDO:0007256	EFO:0000182
lymphoma	2	MONDO:0005062	EFO:0000574
mast cell leukemia	2	MONDO:0020334	EFO:0007359
gastroparesis	2	MONDO:0006769	EFO:1000948
glioma	2	MONDO:0021042	MONDO:0100342

8 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 81.

Phase distribution

Phase	Trials
PHASE3	24
PHASE4	18
PHASE2	17
Not specified	11
PHASE1	9
PHASE2/PHASE3	1
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04150614	PHASE4	RECRUITING	BMT-08: A Comparative Effectiveness Study of Transdermal Granisetron to Ondansetron
NCT07360431	PHASE4	NOT_YET_RECRUITING	Granisetron Combined With Dexamethasone or Metoclopramide for PONV Prevention After Laparoscopic Cholecystectomy
NCT07401745	PHASE4	ACTIVE_NOT_RECRUITING	Occlusal Splint Combined With Granisetron Injection for Management of Myofascial Pain Related to Temporomandibular Disorders
NCT00231478	PHASE4	COMPLETED	A Study of Kytril (Granisetron) in the Prevention of Post-Operative Nausea and Vomiting (PONV) in Pediatric Subjects Undergoing Tonsillectomy or Adenotonsillectomy
NCT00415103	PHASE4	COMPLETED	AMENO-2: Aprepitant Plus Palonosetron Versus Granisetron in the Prevention of Nausea and the Emesis Induced by Chemotherapy in Patients Treated With Haematopoietic Progenitors
NCT01352130	PHASE4	COMPLETED	Granisetron Versus Ondansetron: Comparative Effects on ECG, QTc
NCT01659775	PHASE4	COMPLETED	Phase 4 Trial to Evaluate the Efficacy and Safety of Sancuso Patch in Chemotherapy-induced Nausea and Vomiting Associated With the Administration of Highly Emetogenic Chemotherapy (HEC)
NCT01662687	PHASE4	UNKNOWN	Phase 4 Trial to Evaluate the Efficacy and Safety of Sancuso Patch in CINV (Chemotherapy-induced Nausea and Vomiting) Associated With the Administration of MEC (Moderately Emetogenic Chemotherapy)
NCT02230371	PHASE4	COMPLETED	Study on the Effect of Granisetron on Myofascial Pain in the Orofacial Muscles
NCT02441894	PHASE4	COMPLETED	Combination of Cabazitaxel With Prednisolone With Primary Prophylaxis With PEG-G-CSF in Treatment of Patients With Prostate Cancer
NCT03017391	PHASE4	UNKNOWN	Treatment Algorithm for Nausea and Vomiting in the Palliative Phase
NCT03091881	PHASE4	COMPLETED	Granisetron in Diabetic Parturients Decrease Spinal Induced Hypotension
NCT03180229	PHASE4	COMPLETED	Granisetron Effect on Hemodynamic Changes in Laparoscopic Cholecystectomy
NCT03503292	PHASE4	COMPLETED	Pharmacogenomics and Post-Operative Nausea and Vomiting
NCT04899817	PHASE4	UNKNOWN	Granisteron Versus Metoclopramide in Laparoscopic Cholecystectomy
NCT05434663	PHASE4	UNKNOWN	Safety Study of Repeat Doses of SUSTOL in Adults
NCT05632224	PHASE4	UNKNOWN	Postoperative Nausea and Vomiting in Laparoscopic Abdominal Surgery
NCT06513806	PHASE4	COMPLETED	Granisetron Versus Pethidine in Treatment of Post Spinal Shivering in Cesarean Sections
NCT03817970	PHASE3	ACTIVE_NOT_RECRUITING	Cisplatin Disposition and Kidney Injury
NCT00003213	PHASE3	COMPLETED	Drugs to Reduce the Side Effects of Chemotherapy
NCT00004219	PHASE3	UNKNOWN	Lerisetron Compared With Granisetron in Preventing Nausea and Vomiting in Men Being Treated With Radiation Therapy for Stage I Seminoma
NCT00005024	PHASE3	UNKNOWN	Granisetron to Prevent Nausea and Vomiting After Chemotherapy in Patients With Malignant Disease
NCT00020657	PHASE3	COMPLETED	Comparison of Antiemetic Drugs in Preventing Delayed Nausea After Chemotherapy in Patients With Cancer
NCT00272285	PHASE3	COMPLETED	A Study of Ramosetron Plus DX, Dexamethasone, Compared to Granisetron Plus DX for the Prevention of Vomiting and Nausea
NCT00273468	PHASE3	COMPLETED	To Study the Safety and Effectiveness of a Granisetron Patch to Treat Chemotherapy-Induced Nausea and Vomiting (CINV)
NCT00343460	PHASE3	COMPLETED	APF530 or Aloxi (Palonosetron Hydrochloride) Combined With Dexamethasone in Preventing Nausea and Vomiting in Patients Receiving Chemotherapy for Cancer
NCT00359567	PHASE3	COMPLETED	Comparative Study of Palonosetron With Granisetron as a Control in Patients Receiving Highly Emetogenic Chemotherapy
NCT00475085	PHASE3	COMPLETED	Prevention of Delayed Nausea A Phase III Double-Blind Placebo-Controlled Clinical Trial
NCT00952341	PHASE3	COMPLETED	Aprepitant/MK0869 for Prevention of Chemotherapy Induced Nausea and Vomiting Associated With Cisplatin (0869-169)(COMPLETED)
NCT01499849	PHASE3	COMPLETED	Ph3 Safety/Efficacy Study of Rolapitant for the Prevention of CINV in Subjects Receiving Highly Emetogenic Chemotherapy
NCT01500213	PHASE3	COMPLETED	Ph3 Safety/Efficacy Study of Rolapitant for the Prevention of CINV in Subjects Receiving Highly Emetogenic Chemotherapy
NCT01500226	PHASE3	COMPLETED	Ph 3 Safety/Efficacy Study of Rolapitant for Prevention of CINV in Subjects Receiving Moderately Emetogenic Chemotherapy
NCT01536392	PHASE3	COMPLETED	Oral Ondansetron Versus Transdermal Granisetron (Sancuso) for Women With Cervical, Endometrial or Vaginal Cancer Receiving Pelvic Chemoradiation
NCT01937156	PHASE3	COMPLETED	A Randomized Controlled Trial of SP-01 (Granisetron Transdermal Delivery System) in Chemotherapy-induced Nausea and Vomiting
NCT02106494	PHASE3	COMPLETED	A Prospective, Multicenter, Study of APF530 (Granisetron) SC for Prevention of CINV in Patients Receiving HEC
NCT03483350	PHASE3	UNKNOWN	Comp Granisetron Midazolam Comb in Lap Children
NCT04613726	PHASE3	COMPLETED	The Effect of Intravenous Granisetron and Ondansetron in Patients Undergoing Cesarean Section
NCT04912271	PHASE3	UNKNOWN	Granisetron Transdermal Patch for Prophylaxis of Delayed CINV
NCT04918862	PHASE3	COMPLETED	A COMPARATIVE STUDY BETWEEN 1MG AND 3 MG OF GRANISETRON IN THE PREVENTION OF POSTOPERATIVE NAUSEA AND VOMITING IN STRABISMUS OPHTHALMIC SURGERIES DURING GENERAL ANESTHESIA
NCT05087615	PHASE3	COMPLETED	Effects of Ondansetron, Metoclopramide and Granisetron on Perioperative Nausea and Vomiting in Patients Undergone Bariatric Surgery

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 6 clinical and 22 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).