Page last updated: 2024-12-07

ramosetron

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Ramosetron is a selective 5-HT3 receptor antagonist that is used to prevent nausea and vomiting associated with chemotherapy. It was synthesized by scientists at Yamanouchi Pharmaceutical Company in Japan, and it was first approved for medical use in 1990. Ramosetron is a potent inhibitor of 5-HT3 receptors, which are located in the gastrointestinal tract and play a role in mediating the vomiting reflex. By blocking these receptors, ramosetron prevents the release of serotonin, a neurotransmitter that triggers nausea and vomiting. Ramosetron is effective in preventing nausea and vomiting caused by a variety of chemotherapy regimens, and it is generally well-tolerated. The drug is administered intravenously or orally, and it is typically used in conjunction with other antiemetics. Ramosetron has been the subject of numerous clinical trials, and it has been found to be effective in reducing nausea and vomiting in patients receiving chemotherapy for various types of cancer. Ramosetron is also being studied for its potential therapeutic effects in other conditions, such as irritable bowel syndrome and migraine headaches.'

Cross-References

ID SourceID
PubMed CID108000
CHEMBL ID1643895
CHEBI ID135156
SCHEMBL ID16701
MeSH IDM0193791

Synonyms (34)

Synonym
unii-7zro0sc54y
7zro0sc54y ,
(-)-(r)-1-methylindol-3-yl-4,5,6,7-tetrahydro-5-benzimidazolyl ketone
ramosetron [inn]
nor-ym 060
(-)-(r)-1-methylindol-3-yl-4,5,6,7-tetrahydro-5-benzimidazolyl ketone.
bdbm50334454
gtpl2301
ramosetron
CHEBI:135156
ramosetron (inn)
132036-88-5
D08466
(1-methylindol-3-yl)-[(5r)-4,5,6,7-tetrahydro-3h-benzimidazol-5-yl]methanone
A806353
(r)-(1-methyl-1h-indol-3-yl)(4,5,6,7-tetrahydro-1h-benzo[d]imidazol-6-yl)methanone
CHEMBL1643895 ,
AKOS015896003
ramosetron [who-dd]
ramosetron [mi]
SCHEMBL16701
(r)-(-)-5-[(1-methyl-3-indolyl)carbonyl]-4,5,6,7-tetrahydrobenzimidazole
NTHPAPBPFQJABD-LLVKDONJSA-N
DTXSID0043842
(r)-5-[(1-methylindole-3-yl)carbonyl]-4,5,6,7-tetrahydro-1h-bezimidazole
methanone,(1-methyl-1h-indol-3-yl)[(6r)-4,5,6,7-tetrahydro-1h-benzimidazol-6-yl]-
DB09290
(1-methyl-1h-indol-3-yl)(4,5,6,7-tetrahydro-1h-benzimidazol-6-yl)methanone
(-)-(r)-1-methylindol-3-yl 4,5,6,7-tetrahydro-5-benzimidazolylketone
Q2979523
AR-270/43507766
(1-methylindol-3-yl)-[(5r)-4,5,6,7-tetrahydro-3h-benzimidazol-5-yl]methanone.
R-146
methanone, (1-methyl-1h-indol-3-yl)[(6r)-4,5,6,7-tetrahydro-1h-benzimidazol-6-yl]-

Research Excerpts

Overview

Ramosetron is an enantiopure active pharmaceutical ingredient marketed in Japan since 1996 and later in a few Southeast Asian countries. It is used as an antiemetic for patients receiving chemotherapy. Ramosetron has been shown to reduce PONV in general anesthesia.

ExcerptReferenceRelevance
"Ramosetron is an enantiopure active pharmaceutical ingredient marketed in Japan since 1996 and later in a few Southeast Asian countries predominantly as an antiemetic for patients receiving chemotherapy. "( Direct separation of the enantiomers of ramosetron on a chlorinated cellulose-based chiral stationary phase in hydrophilic interaction liquid chromatography mode.
Cirilli, R; Colombo, M; Ferretti, R; Zanitti, L, 2020
)
2.27
"Ramosetron is a potent and selective serotonin type 3 receptor antagonist. "( Ramosetron for the treatment of irritable bowel syndrome with diarrhea: a systematic review and meta-analysis of randomized controlled trials.
Chen, F; Li, Y; Qi, Q; Zhang, Y; Zuo, X, 2018
)
3.37
"Ramosetron is a new selective 5-hydroxytryptamine type 3 (5-HT3) receptor antagonist that reportedly has more potent antiemetic effects than other 5-HT3 receptor antagonists. "( Effects of ramosetron oral disintegrating tablets on gastric emptying: crossover study using the 13C-acetic acid breath test.
Endo, H; Fujita, K; Goto, A; Gotoh, E; Iida, H; Inamori, M; Koide, T; Kusakabe, A; Maeda, S; Nakajima, A; Nonaka, T; Nosaka, C; Sekino, Y; Takahashi, H; Yoneda, M,
)
1.96
"Ramosetron is a selective serotonergic 5-hydroxy-tryptamine receptor 3 antagonist that is used to prevent and treat postoperative nausea and vomiting. "( Population pharmacokinetics of ramosetron.
Cho, SY; Jeong, S; Lee, SH; Yoo, KY, 2016
)
2.16
"Ramosetron is a relatively new 5-hydroxytryptamine three receptor antagonist with higher binding affinity and more prolonged duration of action compared to ondansetron. "( Effect of ramosetron on QTc interval: a randomised controlled trial in patients undergoing off-pump coronary artery bypass surgery.
Cho, YJ; Choi, EK; Hong, DM; Jeon, Y; Kim, TK; Lim, CW; Min, JJ, 2016
)
2.28
"Ramosetron is a 5-HT₃ antagonist that has been shown to reduce PONV in general anesthesia."( A Randomized Placebo-Controlled Trial of Oral Ramosetron for Prevention of Post Operative Nausea and Vomiting after Intrathecal Morphine in Patients Undergoing Gynecological Surgery.
Amornyotin, S; Chinachoti, T; Noitasaeng, P; Sukantarat, N; Wangnamthip, S; Wongtangman, K, 2016
)
1.41
"Ramosetron is an effective and well-tolerated treatment not only for female IBS patients but also for male patients."( A phase II trial of the novel serotonin type 3 receptor antagonist ramosetron in Japanese male and female patients with diarrhea-predominant irritable bowel syndrome.
Harasawa, S; Hiwatashi, N; Hongo, M; Matsueda, K; Sasaki, D, 2008
)
2.02
"Ramosetron is a newly developed 5-HT3 antagonist with higher receptor affinity and longer duration of action having theoretical advantage over ondansetron in this setting."( Effect of ramosetron on patient-controlled analgesia related nausea and vomiting after spine surgery in highly susceptible patients: comparison with ondansetron.
Choi, YS; Jeon, DH; Kwak, YL; Lee, JY; Shim, JK; Yoon, DH, 2008
)
1.47
"Ramosetron proved to be an effective alternative for the control of CRINV during upper abdominal irradiation with concurrent 5-fluorouracil chemotherapy."( Ramosetron for the prevention of nausea and vomiting during 5-fluorouracil-based chemoradiotherapy for pancreatico-biliary cancer.
Bang, YJ; Chie, EK; Ha, SW; Im, SA; Jang, JY; Kim, K; Kim, SW; Kim, TY; Oh, DY, 2009
)
3.24
"Ramosetron is a new selective 5-hydroxytryptamine type 3 (5-HT(3)) receptor antagonist that reportedly has more potent antiemetic effects compared with other 5-HT(3) receptor antagonists. "( Comparison of ramosetron with ondansetron for prevention of postoperative nausea and vomiting in patients undergoing gynaecological surgery.
Baek, YH; Kim, SC; Kim, SH; Kim, SI; Ok, SY, 2009
)
2.16
"Ramosetron is a selective serotonin 5-HT3 receptor antagonist with an affinity higher than that of the previously available drugs ondansetron, granisetron and tropisetron. "( Ramosetron, a 5-HT3 receptor antagonist for the control of nausea and vomiting.
Rabasseda, X, 2002
)
3.2
"Ramosetron is a safe and effective antiemetic and is more cost-effective than granisetron."( [Preventive effects of ramosetron and granisetron in prevention of gastrointestinal reaction associated with chemotherapeutic agents: a comparative study].
Liu, YP; Shi, J; Teng, YE; Zhang, JD, 2003
)
2.07
"Ramosetron is a selective serotonin receptor antagonist (SSRA) that is approved for the treatment of emetic symptoms induced by cytotoxic drugs in Japan. "( Randomized, double-blind, placebo-controlled, dosed-finding study of the antiemetic effects and tolerability of ramosetron in adults undergoing middle ear surgery.
Fujii, Y; Tanaka, H, 2003
)
1.97
"Ramosetron is a long-lasting and safe antiemetic agent."( Ramosetron versus ondansetron in the prevention of chemotherapy-induced gastrointestinal side effects: A prospective randomized controlled study.
Ai, B; Dong, M; Han, X; He, X; Huang, D; Liu, P; Shi, Y; Yang, S; Zhang, C; Zhou, S, 2007
)
3.23
"Ramosetron is a potent and selective serotonin (5-HT)(3) receptor antagonist that has been shown to affect abnormal colonic function and abdominal pain in animals. "( Pharmacological profile of ramosetron, a novel therapeutic agent for IBS.
Funatsu, T; Hirata, T; Keto, Y; Nakata, M; Sasamata, M, 2007
)
2.08
"Ramosetron is a better antiemetic than granisetron for the long-term prevention of postoperative vomiting in children undergoing general anesthesia for tonsillectomy."( Prevention of vomiting after tonsillectomy in children: granisetron versus ramosetron.
Fujii, Y; Kobayashi, N; Saitoh, Y, 2001
)
1.98
"Ramosetron hydrochloride is a 5-HT3 receptor antagonist, which has an active metabolite (M-1), expected to be useful in the inhibition of chemotherapy-induced nausea and vomiting."( [Analysis of 5-HT3 receptor antagonist, ramosetron hydrochloride, based on receptor occupancy considering its active metabolite].
Iga, T; Ogata, A; Sawada, Y; Sugiura, M; Takayanagi, R; Yamada, Y, 2001
)
1.3

Effects

Ramosetron has been shown to have a very strong effect for preventing postoperative nausea and vomiting (PONV) in previous meta-analyses. It has superior antiemetic activity to ondansetron in adult strabismus surgery patients.

ExcerptReferenceRelevance
"Ramosetron has a significant effect for preventing PONV compared with a placebo, but less than that reported in previous analyses. "( Reevaluation of the effectiveness of ramosetron for preventing postoperative nausea and vomiting: a systematic review and meta-analysis.
Goto, T; Mihara, T; Morita, S; Tojo, K; Uchimoto, K, 2013
)
2.11
"Ramosetron has been shown to have a very strong effect for preventing postoperative nausea and vomiting (PONV) in previous meta-analyses. "( Reevaluation of the effectiveness of ramosetron for preventing postoperative nausea and vomiting: a systematic review and meta-analysis.
Goto, T; Mihara, T; Morita, S; Tojo, K; Uchimoto, K, 2013
)
2.11
"Ramosetron has a significant effect for preventing PONV compared with a placebo, but less than that reported in previous analyses. "( Reevaluation of the effectiveness of ramosetron for preventing postoperative nausea and vomiting: a systematic review and meta-analysis.
Goto, T; Mihara, T; Morita, S; Tojo, K; Uchimoto, K, 2013
)
2.11
"Ramosetron has superior antiemetic activity to ondansetron in adult strabismus surgery patients. "( Ramosetron versus ondansetron for postoperative nausea and vomiting in strabismus surgery patients.
Joo, J; Park, HJ; Park, S; Shin, SY, 2016
)
3.32
"Oral ramosetron has the same anti-anorectic and anti-emetic effects as intravenous granisetron."( Comparative clinical study of the anti-emetic effects of oral ramosetron and injected granisetron in patients with malignant glioma undergoing ACNU chemotherapy.
Hamada, J; Kai, Y; Kochi, M; Kuratsu, J; Makino, K; Morioka, M; Nakamura, H; Yano, S, 2005
)
1.02

Actions

ExcerptReferenceRelevance
"Ramosetron use led to a lower incidence, mild severity of nausea, and reduced use of rescue antiemetic drug after arthroscopic rotator cuff repair during the 6- to 24-h postoperative period than the control."( The effectiveness of ramosetron and ondansetron for preventing postoperative nausea and vomiting after arthroscopic rotator cuff repair: a randomized controlled trial.
Kim, YS; Lee, HJ; Lee, SU, 2020
)
2.32

Treatment

Ramosetron could cause more hard stool and constipation, without severe adverse events. Ramosetron-treated patients showed high rates of global improvement.

ExcerptReferenceRelevance
"Ramosetron-treated patients showed high rates of global improvement."( Effect of ramosetron in female patients with irritable bowel syndrome with diarrhea: a phase III long-term study.
Akiho, H; Fukudo, S; Haruma, K; Hayashi, K; Ida, M; Kinoshita, Y; Nakashima, Y; Okumura, T, 2016
)
1.56
"Treatment with ramosetron could cause more hard stool and constipation, without severe adverse events."( Ramosetron for the treatment of irritable bowel syndrome with diarrhea: a systematic review and meta-analysis of randomized controlled trials.
Chen, F; Li, Y; Qi, Q; Zhang, Y; Zuo, X, 2018
)
2.26

Toxicity

Ramosetron is a long-lasting and safe antiemetic agent. 40% (33/141) experienced at least one adverse event within 24 hours of taking the drug.

ExcerptReferenceRelevance
"The side effect of anticancer agents such as nausea and vomiting frequently interrupt chemotherapy."( [Effect of steroid on antiemetic for side effect of anticancer chemotherapy].
Matsumoto, T; Mikami, T; Momokawa, K; Nakamura, Y; Sakayauchi, T; Sasaki, T; Watanabe, T, 2005
)
0.33
"Data were collected for analysis of the therapeutic effect in 47 cases and for adverse events in 50 cases."( Ramosetron versus ondansetron in the prevention of chemotherapy-induced gastrointestinal side effects: A prospective randomized controlled study.
Ai, B; Dong, M; Han, X; He, X; Huang, D; Liu, P; Shi, Y; Yang, S; Zhang, C; Zhou, S, 2007
)
1.78
"Ramosetron is a long-lasting and safe antiemetic agent."( Ramosetron versus ondansetron in the prevention of chemotherapy-induced gastrointestinal side effects: A prospective randomized controlled study.
Ai, B; Dong, M; Han, X; He, X; Huang, D; Liu, P; Shi, Y; Yang, S; Zhang, C; Zhou, S, 2007
)
3.23
" Of the 460 cycles, adverse events, drug-related adverse events, and serious adverse events occurred in 179 (38."( Safety and efficacy of aprepitant, ramosetron, and dexamethasone for chemotherapy-induced nausea and vomiting in patients with ovarian cancer treated with paclitaxel/carboplatin.
Bae, DS; Choi, CH; Kim, BG; Kim, HJ; Kim, MK; Kim, TJ; Lee, JW; Lee, YY; Park, JY; Yoon, A, 2014
)
0.68
"Triplet therapy using an increased-dose of DEX is suggested to be safe and effective for patients receiving HEC."( Efficacy and safety of an increased-dose of dexamethasone in patients receiving fosaprepitant chemotherapy in Japan.
Akashi, K; Arita, S; Ariyama, H; Baba, E; Komoda, M; Kumagai, H; Kusaba, H; Nagata, K; Nakano, M; Okumura, Y; Takaishi, S; Tamura, S; Uchida, M, 2014
)
0.4
"Postoperative nausea and vomiting is a common side effect of general anesthesia."( Efficacy and safety of ramosetron versus ondansetron for postoperative nausea and vomiting after general anesthesia: a meta-analysis of randomized clinical trials.
Cao, G; Gao, C; Li, B; Lv, F; Wang, F; Wang, H; Wu, G; Xu, L, 2015
)
0.73
"In this retrospective analysis of 10,575 patients who used fentanyl-based intravenous patient-controlled analgesia (IV-PCA) after surgery, we evaluated difference between young and elderly patients on their characteristic of adverse effects."( Postoperative Pain and Intravenous Patient-Controlled Analgesia-Related Adverse Effects in Young and Elderly Patients: A Retrospective Analysis of 10,575 Patients.
Choi, S; Han, DW; Kim, SY; Koh, JC; Lee, J, 2015
)
0.42

Pharmacokinetics

The single-dose pharmacokinetic profile of ramosetron 10 microg is not affected to a clinically relevant degree by paroxetine 20 mg once daily administered for 10 days.

ExcerptReferenceRelevance
"It can be concluded that the single-dose pharmacokinetic profile of ramosetron 10 microg is not affected to a clinically relevant degree by paroxetine 20 mg once daily administered for 10 days."( The effect of paroxetine on the pharmacokinetics, safety, and tolerability of ramosetron in healthy subjects.
den Adel, M; Kadokura, T; Krauwinkel, WJ; Nishida, A; Takeshige, T, 2008
)
0.81
" Pooled data from 50 patients and 479 pharmacokinetic samples were used for population pharmacokinetic analysis using the nonlinear mixed effect modeling program (NONMEM(®))."( Population pharmacokinetics of ramosetron.
Cho, SY; Jeong, S; Lee, SH; Yoo, KY, 2016
)
0.72
"The pharmacokinetic parameter estimates were V1 (l) = 5."( Population pharmacokinetics and prophylactic anti-emetic efficacy of ramosetron in surgical patients.
Choi, BM; Jeong, SW; Lee, EK; Lee, YH; Lim, YJ; Min, KT; Noh, GJ; Seo, JH, 2016
)
0.67

Compound-Compound Interactions

ExcerptReferenceRelevance
"A systematic review and meta-analysis of published randomized controlled trials was performed to update the present evidence about the safety and efficacy of dexamethasone combined with other antiemetics versus single antiemetics for the prevention of postoperative nausea and vomiting after laparoscopic cholecystectomy."( Dexamethasone combined with other antiemetics versus single antiemetics for prevention of postoperative nausea and vomiting after laparoscopic cholecystectomy: An updated systematic review and meta-analysis.
Abushouk, AI; Ahmed, H; Al Nahrawi, S; Attia, A; Awad, K; Elsherbeny, MY; Mustafa, SM, 2016
)
0.43
"Pooled data from 14 RCTs (1542 patients) favored dexamethasone combined with other antiemetics over single antiemetics as a prophylaxis against postoperative nausea and vomiting after laparoscopic cholecystectomy in the early postoperative period (OR = 0."( Dexamethasone combined with other antiemetics versus single antiemetics for prevention of postoperative nausea and vomiting after laparoscopic cholecystectomy: An updated systematic review and meta-analysis.
Abushouk, AI; Ahmed, H; Al Nahrawi, S; Attia, A; Awad, K; Elsherbeny, MY; Mustafa, SM, 2016
)
0.43
"Dexamethasone combined with other antiemetics provided better prophylaxis than single antiemetics against postoperative nausea and vomiting after laparoscopic cholecystectomy."( Dexamethasone combined with other antiemetics versus single antiemetics for prevention of postoperative nausea and vomiting after laparoscopic cholecystectomy: An updated systematic review and meta-analysis.
Abushouk, AI; Ahmed, H; Al Nahrawi, S; Attia, A; Awad, K; Elsherbeny, MY; Mustafa, SM, 2016
)
0.43
"25 mg intravenously) D1, combined with APR (125 mg orally, D1 and 80 mg orally, D2-3) and DEX (12 mg orally or intravenously, D1 and 8 mg orally, D2-4)."( Ramosetron versus Palonosetron in Combination with Aprepitant and Dexamethasone for the Control of Highly-Emetogenic Chemotherapy-Induced Nausea and Vomiting.
Ahn, JS; An, HJ; Kang, JH; Kim, GM; Kim, HJ; Kim, JY; Koo, DH; Kwon, JH; Lee, H; Lee, YG; Park, KU; Seol, YM; Sohn, J; Song, H; Yang, JH; Yun, HJ, 2020
)
2

Dosage Studied

Oral ramosetron at a dosage of 0.5 mg had a significant effect on CFS-induced defecation.

ExcerptRelevanceReference
" YM114 (KAE-393), YM-26103-2, YM-26308-2 (3 x 10(-9) to 3 x 10(-8) M) produced concentration-dependent shifts to the right of the dose-response curves for both 5-HT and 2-methyl-5-HT (2-Me-5-HT)."( Studies on serotonin (5-HT)3-receptor antagonist effects of enantiomers of 4,5,6,7-tetrahydro-1H-benzimidazole derivatives.
Honda, K; Ito, H; Kamato, T; Miyata, K; Suzuki, T, 1995
)
0.29
" Left and right cheek pouches were examined before dosing each day, and on the day following the last treatment."( Two-week oral mucosal irritation study with ramosetron orally disintegrating tablets in Syrian hamsters.
Cummins, HA; Suzuki, H; Tabata, H, 1996
)
0.56
"Suppositories are the preferable dosage form for patients at home or experiencing nausea."( Mucoadhesive suppositories of ramosetron hydrochloride utilizing Carbopol.
Machida, Y; Onishi, H; Yahagi, R, 2000
)
0.6
" Patient preference for the dosage form was also investigated."( [Evaluation of efficacy of ramosetron orally disintegrating tablets and patient preference as to the dosage form in gynecological cancer chemotherapy].
Nakayama, S; Noda, T; Torii, Y, 2001
)
0.61
" The present analysis method should be useful for designing the rational dosage regimen of ramosetron hydrochloride and predicting the duration of its antiemetic activity in a quantitative manner."( [Analysis of 5-HT3 receptor antagonist, ramosetron hydrochloride, based on receptor occupancy considering its active metabolite].
Iga, T; Ogata, A; Sawada, Y; Sugiura, M; Takayanagi, R; Yamada, Y, 2001
)
0.8
" Dosing of fluvoxamine started with an initial morning dose of 50 mg on Day 3, followed by a twice daily (12-h interval) dosing of 50 mg on Days 4-12."( The effect of fluvoxamine on the pharmacokinetics, safety, and tolerability of ramosetron in healthy subjects.
den Adel, M; Kadokura, T; Krauwinkel, WJ; Nishida, A; Takeshige, T, 2008
)
0.57
"This study shows a trend regarding the dose-response relationship for ramosetron to prevent CINV, including delayed emesis."( A Randomized, Double-Blind Pilot Study of Dose Comparison of Ramosetron to Prevent Chemotherapy-Induced Nausea and Vomiting.
Bae, WK; Cho, SH; Chung, IJ; Hwang, JE; Jeong, S; Kang, G; Ki, MS; Kim, JK; Kim, KR; Shim, HJ, 2015
)
0.89
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
indolesAny compound containing an indole skeleton.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 3AHomo sapiens (human)Ki0.00010.00000.74119.9000AID552106
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (7)

Processvia Protein(s)Taxonomy
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3AHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
cleavage furrow5-hydroxytryptamine receptor 3AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (6)

Assay IDTitleYearJournalArticle
AID680934TP_TRANSPORTER: uptake, not inhibited by Verapamil in MBEC4 cell2002The Journal of pharmacy and pharmacology, Aug, Volume: 54, Issue:8
Contribution of P-glycoprotein to efflux of ramosetron, a 5-HT3 receptor antagonist, across the blood-brain barrier.
AID678944TP_TRANSPORTER: uptake in LLC-PK1 cell and LLC-GA5-COL300 cells2002The Journal of pharmacy and pharmacology, Aug, Volume: 54, Issue:8
Contribution of P-glycoprotein to efflux of ramosetron, a 5-HT3 receptor antagonist, across the blood-brain barrier.
AID681556TP_TRANSPORTER: uptake in L cell and LV500 cell2002The Journal of pharmacy and pharmacology, Aug, Volume: 54, Issue:8
Contribution of P-glycoprotein to efflux of ramosetron, a 5-HT3 receptor antagonist, across the blood-brain barrier.
AID552106Binding affinity to human 5HT3A receptor2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.
AID552297Partial agonist activity at human 5HT3A receptor expressed in HEK293 cells assessed as decrease in 100 uM 5-chloroindole-induced increase in intracellular calcium release at 3 uM relative to 5-HT2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.
AID552110Partial agonist activity at human 5HT3A receptor expressed in HEK293 cells at 3 uM relative to 5HT2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (186)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's38 (20.43)18.2507
2000's57 (30.65)29.6817
2010's77 (41.40)24.3611
2020's14 (7.53)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 61.85

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index61.85 (24.57)
Research Supply Index5.67 (2.92)
Research Growth Index4.66 (4.65)
Search Engine Demand Index103.63 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (61.85)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials94 (48.45%)5.53%
Reviews19 (9.79%)6.00%
Case Studies3 (1.55%)4.05%
Observational3 (1.55%)0.25%
Other75 (38.66%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (50)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Prophylactic Effects of Ondansetron, Ramosetron, and Palonosetron on Patient-Controlled Analgesia Related Nausea and Vomiting After Urologic Laparoscopic Surgery [NCT01169805]105 participants (Actual)Interventional2010-08-31Completed
Effects of Ramosetron Orally Disintegrating Tablet on the Prophylaxis of Postdischarge Nausea and Vomiting in High-risk Patients Undergoing Day Surgery Under General Anesthesia [NCT04297293]Phase 4138 participants (Anticipated)Interventional2020-05-12Recruiting
Post-marketing Clinical Study of Ramosetron Hydrochloride (Irribow Tablets) - Double-blind, Parallel-group Comparative Study in Patients (Male) With Diarrhea-predominant Irritable Bowel Syndrome [NCT01225237]Phase 4296 participants (Actual)Interventional2010-10-31Completed
Special Drug Use Surveillance of Irribow® Tablets and Irribow® OD Tablets in Female Patients [NCT02612649]793 participants (Actual)Observational2015-10-01Completed
Comparative Study of Antiemetic Effect of Ramosetron With Combination of Ondansetron and Dexamethasone in Patients Undergoing Laparoscopic Cholecystectomy [NCT02803788]Phase 4100 participants (Anticipated)Interventional2015-07-31Recruiting
The Safety and Efficacy of 5-HT3 Receptor Antagonist (Ramosetron) Versus Psyllium (Agio®) for the Treatment of Fecal Incontinence: Multicenter Randomized Trial (SERAFI) [NCT06166615]Phase 2/Phase 3148 participants (Anticipated)Interventional2023-12-15Not yet recruiting
High-dose Acupuncture for Prevention of Postoperative Nausea and Vomiting in Patients Undergoing Laparoscopic Colorectal Surgery: A Randomized Controlled Pilot Study [NCT02509143]60 participants (Actual)Interventional2015-07-31Completed
[NCT02478645]Phase 4177 participants (Actual)Interventional2015-06-19Completed
A Study About Pharmacokinetic and Pharmacodynamics of Ramosetron in Chemotherapy Induced Nausea and Vomiting [NCT02076529]51 participants (Actual)Interventional2012-10-31Completed
The Efficacy and Safety of Ramosetron in Patients Undergoing Off Pump Coronary Artery Bypass Surgery [NCT02139241]114 participants (Actual)Interventional2013-06-30Completed
Effect of Ramosetron on Heart Rate-corrected QT Interval During Robot-assisted Laparoscopic Prostatectomy With Steep Trendelenburg Position [NCT03232125]54 participants (Actual)Interventional2017-08-01Completed
Effect of Ramosetron on Postoperative Restoration of Bowel Motility After Gynecological Laparoscopic Surgery [NCT02849483]Phase 488 participants (Anticipated)Interventional2016-07-31Recruiting
Comparison of Ramosetron, Aprepitant, and Dexamethasone (RAD) With Palonosetron, Aprepitant, and Dexamethasone (PAD) for Prevention of Nausea and Vomiting Induced by Highly Emetogenic Chemotherapy [NCT02532634]Phase 4292 participants (Actual)Interventional2015-08-19Completed
[NCT01013012]Phase 494 participants (Actual)Interventional2008-01-31Completed
[NCT01041183]120 participants (Anticipated)Interventional2009-11-30Recruiting
Phase III Prospective Randomized Trial Comparing Ramosetron Versus Ondansetron for Radiotherapy Induced Nausea and Vomiting in the Treatment of Gastrointestinal Cancer [NCT00971399]Phase 3172 participants (Anticipated)Interventional2009-09-30Completed
Post-marketing Clinical Study of Ramosetron Hydrochloride (Irribow Tablets) - A Preliminary Study to Evaluate the Co-primary Endpoint in Patients (Male) With Diarrhea-predominant Irritable Bowel Syndrome [NCT00918411]Phase 498 participants (Actual)Interventional2009-06-30Completed
Analgesia Effects of Nalbuphine vs Sulfentanil in Patient-controlled Intravenous Analgesia After Cesarean Section [NCT02604797]80 participants (Anticipated)Interventional2016-01-31Not yet recruiting
Comparison of the Prophylactic Anti-emetic Efficacy of Gabapentin and Ramosetron in Patients Undergoing Laparoscopic Gynecological Surgery [NCT02617121]120 participants (Anticipated)Interventional2015-11-30Not yet recruiting
A Phase II Study to Evaluate the Efficacy and Tolerability of Ramosetron, Aprepitant and Dexamethasone (RAD) in Preventing Cisplatin-induced Nausea and Vomiting in Chemotherapy-naïve Patients With Solid Cancer [NCT01046461]Phase 241 participants (Actual)Interventional2010-01-31Active, not recruiting
Bioequivalence Study of YM060 Orally-disintegrating Tablet and Conventional Tablet - Ingestion Without Water [NCT01392794]Phase 136 participants (Actual)Interventional2011-04-30Completed
Effect of Ramosetron on Bowel Motility and PONV After Laparoscopic Stomach and Colorectal Resection [NCT01427127]Phase 464 participants (Anticipated)Interventional2010-12-31Recruiting
A Randomized Prospective Study of Scheduled Intravenous Ramosetron for the Prevention of Nausea and Vomiting in Hospitalized Patients After Gynecologic Laparoscopy [NCT02011659]Phase 3128 participants (Anticipated)Interventional2013-11-30Recruiting
The Effect of Additional Administration of Ramosetron on Late PONV (Postoperative Nausea and Vomiting) in Patients Undergoing Breast Surgery [NCT05326360]Phase 4144 participants (Actual)Interventional2020-12-17Completed
Comparison of Ramosetron With Ondansetron for Prevention of Intrathecal Morphine Induced Nausea and Vomiting After Primary Total Knee Arthroplasty: A Randomized Control Trial [NCT02830906]Phase 399 participants (Actual)Interventional2014-04-30Completed
The Effect of Multimodal Anti-emetic Protocol on Postoperative Nausea and Vomiting After Total Knee Arthroplasty [NCT01102491]Phase 4153 participants (Actual)Interventional2009-09-30Completed
Bioequivalence Study of YM060 Orally-disintegrating Tablet and Conventional Tablet - Ingestion With Water - [NCT01394653]Phase 136 participants (Actual)Interventional2011-07-31Completed
A Double-blind, Parallel-group, Comparative Study in Female Patients With Diarrhea-predominant Irritable Bowel Syndrome [NCT01870895]Phase 3577 participants (Actual)Interventional2013-02-28Completed
Comparison of Ramosetron Pre-treatment Time for Postoperative Nausea and Vomiting (PONV) and QTc Prolongation [NCT03278522]Phase 464 participants (Actual)Interventional2017-07-01Completed
A Randomized Double Blind Study to Evaluate Efficacy of Ramosetron and Palonosetron for Prevention of Postoperative Nausea and Vomiting After Gynaecological Laparoscopic Surgery [NCT01476280]100 participants (Actual)Interventional2011-05-31Completed
A Long Term Study of YM060 in Female Patients With Diarrhea-predominant Irritable Bowel Syndrome [NCT01736423]Phase 3151 participants (Actual)Interventional2012-09-30Completed
Prospective, Single-arm Phase 2 Trial to Evaluate Efficacy and Safety of Ramosetron in the Setting of Hematopoietic Stem Cell Transplantation for Hematologic Malignancies [NCT01788605]Phase 265 participants (Anticipated)Interventional2014-08-31Recruiting
[NCT02869984]Early Phase 1100 participants (Anticipated)Interventional2016-08-31Not yet recruiting
To Assess the Efficacy and Safety of Ramosetron, Aprepitant and Dexamethasone Therapy vs Ondansetron, Aprepitant and Dexamethasone Therapy for Preventing of Nausea and Vomiting in Highly Emetogenic Chemotherapy (ROAD Study) [NCT01536691]Phase 3338 participants (Anticipated)Interventional2011-06-30Recruiting
[NCT01806948]Phase 296 participants (Actual)Interventional2013-04-30Completed
A Double-blind, Randomized, Parallel, Comparative Study to Evaluate the Efficacy and Safety of Ramosetron Plus Dexamethasone Injection for the Prevention of Chemotherapy-Induced Vomiting and Nausea [NCT00272285]Phase 3287 participants (Actual)Interventional2006-01-31Completed
Phase 4 Study of Nasea(R)/Ramosetron Inj.as Anti-emetics in the Patients Undergoing Facial Bone Fracture Operations [NCT01637545]Phase 449 participants (Actual)Interventional2011-12-31Terminated(stopped due to Principal Investigator is away on business)
Effects of Different Kinds, Different Doses of 5-HT3 Receptor Antagonists on Prevention of Hypotension After Spinal Anesthesia [NCT01669213]100 participants (Anticipated)Interventional2012-08-31Active, not recruiting
Phase II Study of YM060 - Double-blind, Parallel-group Comparative Study in Patients (Female) With Diarrhea-predominant Irritable Bowel Syndrome [NCT01274000]Phase 2409 participants (Actual)Interventional2010-11-30Completed
[NCT01825733]196 participants (Actual)Interventional2011-08-31Completed
Postoperative Nausea and Vomiting: Ramosetron Plus Aprepitant vs Palonosetron Plus Aprepitant [NCT02597907]88 participants (Actual)Interventional2014-07-31Completed
Effect of Ramosetron on Post-discharge Nausea and Vomiting in Patients Undergoing Gynecologic Surgery Through a Day-surgery Center [NCT03409835]100 participants (Anticipated)Interventional2018-03-01Recruiting
Real-time Decision Support for Postoperative Nausea and Vomiting (PONV) Prophylaxis [NCT02625181]27,034 participants (Actual)Interventional2016-07-31Completed
Safety & Efficacy of 5-HT3 Receptor Antagonist (Ramosetron) Versus Loperamide for the Treatment of Low Anterior Resection Syndrome (RALLARS): Multicenter Randomized Controlled Trial [NCT05577845]212 participants (Anticipated)Interventional2023-03-27Recruiting
[NCT02478047]240 participants (Anticipated)Interventional2015-06-30Not yet recruiting
The Comparison Between Epidural and Intravenous Patient-controlled Analgesia for Laparoscopic Gastrectomy [NCT02444897]Phase 360 participants (Actual)Interventional2013-09-30Completed
Anti Emetic Efficacy of Combination of Ramosetron and Premixture of Naloxone With Patient-controlled Analgesia After Gynecologic Surgery [NCT02416115]90 participants (Actual)Interventional2014-07-31Completed
[NCT03017222]80 participants (Actual)Interventional2015-09-07Completed
Safety and Efficacy of Aprepitant, Ramosetron, and Dexamethasone for Chemotherapy-Induced Nausea and Vomiting in Patients With Ovarian Cancer Treated With Taxane/Carboplatin [NCT01012336]Phase 289 participants (Actual)Interventional2010-05-31Completed
[NCT02480088]Phase 4300 participants (Actual)Interventional2014-09-22Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01012336 (1) [back to overview]Efficacy of the Aprepitant/Ramosetron/Dexamethasone Regimen in Terms of the Proportion of Patients With a Complete Response (CR) During the 120 Hour Following Initiation of Chemotherapy.
NCT01102491 (1) [back to overview]Incidence of Nausea and Vomiting
NCT02597907 (1) [back to overview]The Incidence of Postoperative Nausea and Vomiting
NCT02625181 (4) [back to overview]Adherence to PONV Guidelines
NCT02625181 (4) [back to overview]PONV Incidence: Number of Participants With Postoperative Nausea and Vomiting
NCT02625181 (4) [back to overview]The Number of Prophylactic Interventions for PONV
NCT02625181 (4) [back to overview]Time to Discharge From the Postanesthesia Care Unit (PACU)

Efficacy of the Aprepitant/Ramosetron/Dexamethasone Regimen in Terms of the Proportion of Patients With a Complete Response (CR) During the 120 Hour Following Initiation of Chemotherapy.

Complete Response is defined as No vomiting with no rescue therapy. These response criteria will be applied to the following time periods: Overall: from 0 (chemotherapy initiation) to the morning of day 6, Acute: 0 to 24 hours following the initiation of chemotherapy, Delayed: 25 hours to the morning of day 6(D6). (NCT01012336)
Timeframe: 120 hours

InterventionPercentage of Participants (Number)
Aprepitant89.4

[back to top]

Incidence of Nausea and Vomiting

outcomes assessor who is blinded to randomization assessed the incidence of postoperative nausea which was defined as subjectively unpleasant sensation associated with awareness of the urge to vomit and an emetic episode and vomiting (NCT01102491)
Timeframe: within 48 hours after surgery

Interventionparticipants (Number)
Ramosetron Prophylaxis25
Control32

[back to top]

The Incidence of Postoperative Nausea and Vomiting

The incidence of postoperative nausea and vomiting during 24 hours postoperatively (NCT02597907)
Timeframe: 24 hours

InterventionParticipants (Count of Participants)
Aprepitant Plus Palonosetron5
Aprepitant Plus Ramosetron18

[back to top]

Adherence to PONV Guidelines

PONV guideline adherence: percentage of patients who received the exact number of prophylactic interventions for PONV that were recommended by the decision support. (NCT02625181)
Timeframe: A specific time frame on the day of surgery: the start of admission at the holding room to the end of the anesthetic case

InterventionParticipants (Count of Participants)
Baseline Measurement666
CDS Email Recommendations5260
CDS Email + Real TIme Recommenations5863

[back to top]

PONV Incidence: Number of Participants With Postoperative Nausea and Vomiting

The occurrence of PONV, as defined by the administration of antiemetics in the PACU between admission to PACU and discharge from PACU. (NCT02625181)
Timeframe: PACU recovery period

InterventionParticipants (Count of Participants)
Baseline Measurement139
CDS Email Recommendations1323
CDS Email + Real TIme Recommenations1343

[back to top]

The Number of Prophylactic Interventions for PONV

the absolute number of prophylactic interventions applied between the admission of the patient in the holding room until admission to the PACU. (NCT02625181)
Timeframe: A specific time frame on the day of surgery: from the start of admission at the holding room to the end of the anesthetic case

Interventionprophylactic antiemetics administered (Mean)
Baseline Measurement2.196
CDS Email Recommendations2.176
CDS Email + Real TIme Recommenations2.129

[back to top]

Time to Discharge From the Postanesthesia Care Unit (PACU)

This is the number of minutes from admission to the PACU until discharge, assessed up to 2 days (NCT02625181)
Timeframe: A specific time frame on the day of surgery: from the start of admission to the PACU to discharge from the PACU

Interventionminutes (Mean)
Baseline Measurement266
CDS Email Recommendations264
CDS Email + Real TIme Recommenations266

[back to top]