Compounds > ajm300
Page last updated: 2024-11-11

ajm300

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

Description

AJM300: an alpha4 integrin antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9872780
SCHEMBL ID10329624
MeSH IDM000594816

Synonyms (28)

Synonym
D09799
carotegrast methyl (jan)
carotegrast methyl
unii-oyk17dyo9m
401905-67-7
oyk17dyo9m ,
l-phenylalanine, n-(2,6-dichlorobenzoyl)-4-(6-(dimethylamino)-1,4-dihydro-1-methyl-2,4- dioxo-3(2h)-quinazolinyl)-, methyl ester
carotegrast methyl [who-dd]
carotegrast methyl [jan]
l-phenylalanine, n-(2,6-dichlorobenzoyl)-4-(6-(dimethylamino)-1,4-dihydro-1-methyl-2,4-dioxo-3(2h)-quinazolinyl)-, methyl ester
SCHEMBL10329624
DTXSID60193189
ajm-300
ajm300
gtpl10510
carogra
Q27285918
MS-30291
(2s)-2-[(2,6-dichlorobenzoyl)amino]-3-[4-(1-methyl-2,4-dioxoquinazolin-3-yl)phenyl]propanoic acid
methyl (2s)-2-[(2,6-dichlorobenzoyl)amino]-3-[4-[6-(dimethylamino)-1-methyl-2,4-dioxoquinazolin-3-yl]phenyl]propanoate
methyl (2s)-2-[(2,6-dichlorobenzoyl)amino]-3-[4-[6-
(dimethylamino)-1-methyl-2,4-dioxoquinazolin-3-
yl]phenyl]propanoate
CS-0086113
HY-124290
AKOS040751036
methyl (2s)-2-[(2,6-dichlorophenyl)formamido]-3-{4-[6-(dimethylamino)-1-methyl-2,4-dioxo-1,2,3,4-tetrahydroquinazolin-3-yl]phenyl}propanoate
methyl (2s)-2-[(2,6-dichlorobenzoyl)amino]-3-[4-[6- (dimethylamino)-1-methyl-2,4-dioxoquinazolin-3- yl]phenyl]propanoate

Research Excerpts

Overview

AJM300 is an oral, small-molecule α4-integrin antagonist. It reduces inflammation by blocking leucocyte trafficking.

ExcerptReferenceRelevance
"AJM300 is an oral, small-molecule α4-integrin antagonist. "( AJM300 (carotegrast methyl), an oral antagonist of α4-integrin, as induction therapy for patients with moderately active ulcerative colitis: a multicentre, randomised, double-blind, placebo-controlled, phase 3 study.
Hibi, T; Hirai, F; Ishida, T; Ishiguro, Y; Kajioka, T; Kanke, K; Kishida, S; Kobayashi, K; Matsuoka, K; Miura, Y; Mizusawa, H; Nakajima, K; Ohmori, T; Ohta, A; Watanabe, K; Watanabe, M, 2022)		3.61
"AJM300 is an oral antagonist of α4-integrin that reduces inflammation by blocking leucocyte trafficking. "( AJM300, a novel oral antagonist of α4-integrin, sustains an increase in circulating lymphocytes: A randomised controlled trial in healthy male subjects.
Fukase, H; Furuie, H; Ikeda, N; Kajioka, T; Oikawa, I, 2020)		3.44

Treatment

ExcerptReferenceRelevance
"Oral treatment with AJM300 dose-dependently inhibited lymphocyte homing to Peyer's patches and increased the peripheral lymphocyte count in the same dose range."( Oral treatment with a novel small molecule alpha 4 integrin antagonist, AJM300, prevents the development of experimental colitis in mice.
Andou, A; Dohi, T; Eda, H; Ejima, C; Kageyama, S; Miyazawa, T; Nakayama, A; Sugiura, T, 2013)		0.94

Dosage Studied

The maximal and 24-h sustained pharmacodynamic effects were demonstrated at the 960-mg dosage. Oral administration of AJM300 3 times daily for 6 days was also found to be safe and well tolerated.

ExcerptRelevanceReference
" A significant but transient increase in lymphocyte count was observed after AJM300 dosing at all dosages tested compared with the placebo."( AJM300, a novel oral antagonist of α4-integrin, sustains an increase in circulating lymphocytes: A randomised controlled trial in healthy male subjects.
Fukase, H; Furuie, H; Ikeda, N; Kajioka, T; Oikawa, I, 2020)		2.23
"The maximal and 24-h sustained pharmacodynamic effects were demonstrated at the 960-mg dosage after oral administration of AJM300 3 times daily for 6 days, which was also found to be safe and well tolerated."( AJM300, a novel oral antagonist of α4-integrin, sustains an increase in circulating lymphocytes: A randomised controlled trial in healthy male subjects.
Fukase, H; Furuie, H; Ikeda, N; Kajioka, T; Oikawa, I, 2020)		2.21
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's4 (36.36)24.3611
2020's7 (63.64)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 31.54

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index31.54 (24.57)
Research Supply Index2.77 (2.92)
Research Growth Index4.76 (4.65)
Search Engine Demand Index36.32 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (31.54)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (36.36%)5.53%
Reviews4 (36.36%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other3 (27.27%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
mesalamine
Mesalamine: An anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE. (From Martindale, The Extra Pharmacopoeia, 30th ed). mesalamine : A monohydroxybenzoic acid that is salicylic acid substituted by an amino group at the 5-position.		4.7211amino acid;
aromatic amine;
monocarboxylic acid;
monohydroxybenzoic acid;
phenols		non-steroidal anti-inflammatory drug
carbostyril
Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.. quinolin-2(1H)-one : A quinolone that is 1,2-dihydroquinoline substituted by an oxo group at position 2.		3.2510monohydroxyquinoline;
quinolone		bacterial xenobiotic metabolite
phenylalanine
Phenylalanine: An essential aromatic amino acid that is a precursor of MELANIN; DOPAMINE; noradrenalin (NOREPINEPHRINE), and THYROXINE.. L-phenylalanine : The L-enantiomer of phenylalanine.. phenylalanine : An aromatic amino acid that is alanine in which one of the methyl hydrogens is substituted by a phenyl group.		9.58104amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
phenylalanine;
proteinogenic amino acid		algal metabolite;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
Escherichia coli metabolite;
human xenobiotic metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		3.2310pyrrole;
secondary amine
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		3.6411azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
bromfenac
bromfenac: bromfenac sodium is the active cpd; structure in first source. bromfenac : Amfenac in which the the hydrogen at the 4 position of the benzoyl group is substituted by bromine. It is used for the management of ocular pain and treatment of postoperative inflammation in patients who have undergone cataract extraction. It was withdrawn from the US market in 1998, following concerns over off-label abuse and hepatic failure.		2.3110aromatic amino acid;
benzophenones;
organobromine compound;
substituted aniline		non-narcotic analgesic;
non-steroidal anti-inflammatory drug
moxifloxacin
Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents.		3.811aromatic ether;
cyclopropanes;
fluoroquinolone antibiotic;
pyrrolidinopiperidine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug
pulmicort
Budesonide: A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS.. budesonide : A glucocorticoid steroid having a highly oxygenated pregna-1,4-diene structure. It is used mainly in the treatment of asthma and non-infectious rhinitis and for treatment and prevention of nasal polyposis.		3.231011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
cyclic acetal;
glucocorticoid;
primary alpha-hydroxy ketone		anti-inflammatory drug;
bronchodilator agent;
drug allergen
tofacitinib
tofacitinib : A pyrrolopyrimidine that is pyrrolo[2,3-d]pyrimidine substituted at position 4 by an N-methyl,N-(1-cyanoacetyl-4-methylpiperidin-3-yl)amino moiety. Used as its citrate salt to treat moderately to severely active rheumatoid arthritis.		3.2310N-acylpiperidine;
nitrile;
pyrrolopyrimidine;
tertiary amino compound		antirheumatic drug;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
ccx282-b
CCX282-B: antagonist of CCR9 chemokine receptor		3.1910
oxadiazoles
Oxadiazoles: Compounds containing five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom which exist in various regioisomeric forms.		3.2510
piperidines
Piperidines: A family of hexahydropyridines.		3.2310
laquinimod
[no description available]		3.2510aromatic amide
ConditionIndicatedRelationship StrengthStudiesTrials
Colitis Gravis
[description not available]		0751
Nasopharyngitis
Inflammation of the NASOPHARYNX, usually including its mucosa, related lymphoid structure, and glands.		04.7211
Colitis, Ulcerative
Inflammation of the COLON that is predominantly confined to the MUCOSA. Its major symptoms include DIARRHEA, rectal BLEEDING, the passage of MUCUS, and ABDOMINAL PAIN.		0751
Electrocardiogram QT Prolonged
[description not available]		03.811
Long QT Syndrome
A condition that is characterized by episodes of fainting (SYNCOPE) and varying degree of ventricular arrhythmia as indicated by the prolonged QT interval. The inherited forms are caused by mutation of genes encoding cardiac ion channel proteins. The two major forms are ROMANO-WARD SYNDROME and JERVELL-LANGE NIELSEN SYNDROME.		03.811
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.0810
Bowel Diseases, Inflammatory
[description not available]		03.9120
Inflammatory Bowel Diseases
Chronic, non-specific inflammation of the GASTROINTESTINAL TRACT. Etiology may be genetic or environmental. This term includes CROHN DISEASE and ULCERATIVE COLITIS.		03.9120