lafutidine: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
ID Source | ID |
---|---|
PubMed CID | 5282136 |
CHEMBL ID | 1742461 |
CHEBI ID | 31759 |
SCHEMBL ID | 362540 |
MeSH ID | M0206802 |
Synonym |
---|
protecadin |
frg-8813 |
lafutidine |
stogar |
(+-)-2-(furfurylsulfinyl)-n-(4-(4-(piperidinomethyl)-2-pyridyl)oxy-(z)-2-butenyl)acetamide |
(+-)-2-(furfurylsulfinyl)-n-((z)-4-((4-(piperidinomethyl)-2-pyridyl)oxy)-2-butenyl) acetamide |
lafutidine [inn] |
acetamide, 2-((2-furanylmethyl)sulfinyl)-n-(4-((4-(1-piperidinylmethyl)-2-pyridinyl)oxy)-2-butenyl)-, (z)- |
n-(4-(4-piperidinylmethyl)pyridyl-2-oxy)butenyl-2-(furfurylsulfinyl)acetamide |
D01131 |
protecadin (tn) |
lafutidine (jp17/inn) |
118288-08-7 |
NCGC00164550-01 |
frg 8813 |
L001355 |
AKOS005146275 |
2-(furan-2-ylmethylsulfinyl)-n-[(z)-4-[4-(piperidin-1-ylmethyl)pyridin-2-yl]oxybut-2-enyl]acetamide |
dtxsid0046434 , |
dtxcid8026434 |
cas-118288-08-7 |
tox21_112179 |
CHEMBL1742461 |
S2065 |
206449-93-6 |
rac lafutidine |
49S4O7ADLC , |
(+/-)-2-(furfurylsulfinyl)-n-((z)-4-((4-(piperidinomethyl)-2-pyridyl)oxy)-2-butenyl) acetamide |
lafutidine [jan] |
lafutidine [mart.] |
lafutidine [who-dd] |
lafutidine, (+/-)- |
HY-B0160 |
CS-1992 |
MLS006011259 |
smr002529578 |
NCGC00263530-01 |
tox21_112179_1 |
SCHEMBL362540 |
(z)-2-((furan-2-ylmethyl)sulfinyl)-n-(4-((4-(piperidin-1-ylmethyl)pyridin-2-yl)oxy)but-2-en-1-yl)acetamide |
F0001-2391 |
AC-23354 |
AB01565815_02 |
J-521629 |
CHEBI:31759 |
lafutidine, >=98% (hplc) |
lafutidine [inn:jan:who-dd] |
unii-49s4o7adlc |
SW219706-1 |
DB12770 |
Q582556 |
HMS3884D03 |
118288-08-7 (free base) |
lafutidine free base |
CCG-269024 |
acetamide, 2-[(2-furanylmethyl)sulfinyl]-n-[(2z)-4-[[4-(1-piperidinylmethyl)-2-pyridinyl]oxy]-2-buten-1-yl]- |
(z)-lafutidine |
STARBLD0049801 |
L0341 |
F77861 |
Lafutidine appears to be a promising addition to histamine H1-receptor antagonist therapy for the treatment of chronic urticaria. It has a sensitizing effect on capsaicin-sensitive afferent neurons (CSAN) Lafutidine is a new H2-blocker in India claimed to be more potent and effective than existing H2 blockers.
Excerpt | Reference | Relevance |
---|---|---|
"Lafutidine has a high endoscopic healing rate and improves symptoms of heartburn in patients with mild reflux esophagitis. " | ( A double-blind, controlled study comparing lafutidine with placebo and famotidine in Japanese patients with mild reflux esophagitis. Haruma, K; Kinoshita, Y; Kusano, M; Ohara, S, 2010) | 2.07 |
"Lafutidine has a high endoscopic healing rate and improves symptoms of heartburn in patients with mild reflux esophagitis. " | ( A double-blind, controlled study comparing lafutidine with placebo and famotidine in Japanese patients with mild reflux esophagitis. Haruma, K; Kinoshita, Y; Kusano, M; Ohara, S, 2010) | 2.07 |
Excerpt | Reference | Relevance |
---|---|---|
"The lafutidine-induced increase of [3H]-labeled mucin in the corpus was completely blocked by either NG-nitro-L-arginine (10[-5] M) or 2-(4-carboxyphenyl)-4,4,5,5-tetramethylimidazolne-1-oxyl-3-oxide (10[-5] M)." | ( Lafutidine-induced stimulation of mucin biosynthesis mediated by nitric oxide is limited to the surface mucous cells of rat gastric oxyntic mucosa. Hotta, K; Ichikawa, T; Ishihara, K; Saigenji, K, 1998) | 2.22 |
Treatment with lafutidine (a new type of antagonist of the histamine H(2) receptor) was suggested to interact with capsaicin-sensitive neurons in vivo. Lafutidine pretreatment before WRS caused a significant increase in serum CGRP concentration compared with famotidine.
Excerpt | Reference | Relevance |
---|---|---|
"Lafutidine pretreatment before WRS caused a significant increase in serum CGRP concentration compared with famotidine (lafutidine, 86.64 +/- 9.52 pg/mL; famotidine, 47.55 +/- 4.35 pg/mL; control, 58.43 +/- 6.07 pg/mL)." | ( Lafutidine, a novel histamine H2-receptor antagonist, increases serum calcitonin gene-related peptide in rats after water immersion-restraint stress. Ishihara, S; Kawashima, K; Kazumori, H; Kinoshita, Y; Ortega-Cava, CF; Rumi, MA; Sato, H; Yuki, M, 2003) | 2.48 |
"Treatment with lafutidine (a new type of antagonist of the histamine H(2) receptor), which was suggested to interact with capsaicin-sensitive neurons in vivo, also showed both stimulatory and inhibitory effects on capsaicin-induced contraction depending on the concentrations." | ( Modifications of capsaicin-sensitive neurons in isolated guinea pig ileum by [6]-gingerol and lafutidine. Horie, S; Murayama, T; Someya, A; Yamamoto, H, 2003) | 0.88 |
Excerpt | Reference | Relevance |
---|---|---|
" The aim of this study was to compare the pharmacokinetic and pharmacodynamic properties of lafutidine and famotidine following postprandial oral administration." | ( Pharmacokinetic and pharmacodynamic properties of lafutidine after postprandial oral administration in healthy subjects: comparison with famotidine. Hayato, S; Ikawa, K; Morikawa, N; Shimatani, T; Tazuma, S, 2007) | 0.81 |
Excerpt | Reference | Relevance |
---|---|---|
" Comparison of the parenteral and enteral potencies indicated that FRG-8813 has a lower bioavailability than famotidine and cimetidine in rats and dogs." | ( Gastric antisecretory effect of FRG-8813, a new histamine H2 receptor antagonist, in rats and dogs. Chida, Y; Inaba, N; Ohnishi, H; Onodera, S; Shibata, M; Yamaura, T, 1993) | 0.29 |
" The proposed method enables the unambiguous identification and quantification of lafutidine for pharmacokinetic, bioavailability or bioequivalence studies." | ( Simple, sensitive and rapid LC-ESI-MS method for the quantitation of lafutidine in human plasma--application to pharmacokinetic studies. Chen, WD; Li, H; Liang, Y; Liu, XD; Wang, GJ; Xie, L; Xiong, Y, 2006) | 0.79 |
" Thus, it may be useful for prolonged drug release in stomach to improve the bioavailability and reduced dosing frequency." | ( Gastroretentive mucoadhesive tablet of lafutidine for controlled release and enhanced bioavailability. Patil, S; Talele, GS, 2015) | 0.69 |
Lafutidine at clinical dosage increases plasma CGRP and the somatostatin.
Class | Description |
---|---|
organic molecular entity | Any molecular entity that contains carbon. |
[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] |
Pathway | Proteins | Compounds |
---|---|---|
Lafutidine H2-Antihistamine Action | 10 | 12 |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
acetylcholinesterase | Homo sapiens (human) | Potency | 36.0815 | 0.0025 | 41.7960 | 15,848.9004 | AID1347395; AID1347397; AID1347398 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 17.3768 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 26.6032 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 16 (14.95) | 18.2507 |
2000's | 52 (48.60) | 29.6817 |
2010's | 30 (28.04) | 24.3611 |
2020's | 9 (8.41) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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 strong demand-to-supply ratio for research on this compound.
| This Compound (46.77) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 29 (25.89%) | 5.53% |
Reviews | 3 (2.68%) | 6.00% |
Case Studies | 3 (2.68%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 77 (68.75%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
An Open-label, Multiple-dose, Single-arm, Phase 1 Study to Evaluate the Drug-drug Interaction and Safety of Lafutidine and Irsogladine Maleate in Healthy Adult Volunteers [NCT02581696] | Phase 1 | 24 participants (Actual) | Interventional | 2015-08-31 | Completed | ||
"Effect of Orally Administered Two Successive Doses of PPIs and/ or H2RAs Without or With a Prokinetic Drug, on the Intragastric pH and Volume and Bile Refluxate in Adults Patients Undergoing Elective Surgery." [NCT02703896] | Phase 4 | 1,920 participants (Actual) | Interventional | 2012-01-31 | Completed | ||
Pharmacokinetic Properties and Effect of Food on Pharmacokinetic Properties of the Oral Lafutidine Tablets in Healthy Chinese Subjects [NCT02658864] | Phase 1 | 12 participants (Actual) | Interventional | 2005-04-30 | Completed | ||
[NCT02759224] | Phase 1 | 34 participants (Actual) | Interventional | 2016-04-15 | Completed | ||
Proton Pump Inhibitors and the Risk of Hospitalization for Community-acquired Pneumonia: Replicated Cohort Studies With Meta-analysis [NCT02555852] | 4,238,504 participants (Actual) | Observational | 2011-09-30 | Completed | |||
Verification Study on Lafutidine in Mild Reflux Oesophagitis - Double Blind Controlled Study With Famotidine - [NCT00229424] | Phase 3 | 325 participants | Interventional | 2005-04-30 | Completed | ||
A Multi-center, Randomized, Double-blind Phase III Clinical Trial to Assess and Compare to the Efficacy and Safety of Lafutidine, Famotidine and Omeprazole-referenced in Koran Erosive Esophagitis Patients [NCT01499368] | Phase 3 | 495 participants (Actual) | Interventional | 2011-11-30 | Completed | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |