Page last updated: 2024-11-10

rokitamycin

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

Description

rokitamycin: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5282211
CHEMBL ID1908350
CHEBI ID32103
SCHEMBL ID136367
MeSH IDM0103591

Synonyms (44)

Synonym
tms-19-q ds 200
rokicid
tms-19q
rokital
rokitamycin
ricamycin
((4r,5s,6s,7r,9r,10r,11e,13e,16r)-7-(formylmethyl)-4,10-dihydroxy-5-methoxy-9,16-dimethyl-2-oxooxacyclohexadeca-11,13-dien-6-yl)-3,6-dideoxy-4-o-(2,6-dideoxy-3-c-methyl-alpha-l-ribo-hexopyranosyl)-3-(dimethylamino)-beta-d-glucopyranoside 4''-butyrate 3''-
propionylleucomycin
brn 5220127
tms 19q
rokitamycinum [latin]
3''-o-propionylleucomycin a5
rokitamycin [inn:jan]
ccris 5267
leucomycin v, 4b-butanoate 3b-propanoate
leucomycin v, 4(sup b)-butanoate 3(sup b)-propanoate
rokitamicina [spanish]
rokitamycine [french]
((4r,5s,6s,7r,9r,10r,11e,13e,16r)-7-(formylmethyl)-4,10-dihydroxy-5-methoxy-9,16-dimethyl-2-oxooxacyclohexadeca-11,13-dien-6-yl)-3,6-dideoxy-4-o-(2,6-dideoxy-3-c-methyl-alpha-l-ribo-hexopyranosyl)-3-(dimethylamino)-beta-d-glucopyranoside 4'-butyrate 3'-pr
rokitamycin (jan/inn)
74014-51-0
D01897
ricamycin (tn)
[(2s,3s,4r,6s)-6-[(2r,3s,4r,5r,6s)-6-[[(4r,5s,6s,7r,9r,10r,11e,13e,16r)-4,10-dihydroxy-5-methoxy-9,16-dimethyl-2-oxo-7-(2-oxoethyl)-1-oxacyclohexadeca-11,13-dien-6-yl]oxy]-4-(dimethylamino)-5-hydroxy-2-methyloxan-3-yl]oxy-2,4-dimethyl-4-propanoyloxyoxan-3
rokitamycinum
rokitamicina
rokitamycine
AKOS016010142
zpt03uem0e ,
unii-zpt03uem0e
3''-propionylleucomycin a5
CHEMBL1908350
SCHEMBL136367
rokitamycin [inn]
rokitamycin [jan]
rokitamycin [mi]
rokitamycin [mart.]
rokitamycin [who-dd]
rokitamycin, antibiotic for culture media use only
R-6900
DTXSID6023521
CHEBI:32103
Q3940221
DB13409

Research Excerpts

Overview

Rokitamycin is a semisynthetic macrolide with a lactonic ring with 16 atoms. It shows anti-bacterial action at concentrations near to MIC.

ExcerptReferenceRelevance
"Rokitamycin is a macrolide antibiotic, recently entered into clinical use. "( Inhibitory and bactericidal activity of rokitamycin against Helicobacter pylori and morphological alterations.
Braga, PC; Brenciaglia, MI; Fornara, AM; Scaltrito, MM, 1996
)
2
"Rokitamycin (RKM) is an orally active 16-membered-ring macrolide; there are no reports of specific investigations of these activities in the literature."( Effects of rokitamycin on phagocytosis and release of oxidant radicals of human polymorphonuclear leukocytes.
Braga, PC; Dal Sasso, M; Fonti, E; Ghessi, A; Maci, S,
)
1.24
"Rokitamycin is a semisynthetic macrolide with a lactonic ring with 16 atoms, showing anti-bacterial action at concentrations near to MIC. "( [Rokitamycin in odontostomatology. Controlled study of doses].
Carbone, V; Fornaseri, C; Giangrandi, D; Giordano, M; Mortellaro, C, 1997
)
2.65
"Rokitamycin is a new 16-membered macrolide antibiotic."( Impact of rokitamycin, a new 16-membered macrolide, on serum theophylline.
Cazzola, M; Matera, MG; Paternò, E; Rossi, F; Santangelo, G; Scaglione, F, 1991
)
1.41

Toxicity

ExcerptReferenceRelevance
"Although it is well known that a variety of antibacterials may incidentally cause malignant arrhythmia, the list of drugs causing arrhythmia and the impact of these adverse effects are still uncertain."( Generating signals of drug-adverse effects from prescription databases and application to the risk of arrhythmia associated with antibacterials.
Bagnardi, V; Botteri, E; Carobbio, A; Corrao, G; Falcone, C; Leoni, O; Zambon, A, 2005
)
0.33

Pharmacokinetics

Rokitamycin was absorbed quickly with Tmax for all doses around 30 min after drug intake.

ExcerptReferenceRelevance
" Rokitamycin was absorbed quickly with Tmax for all doses around 30 min after drug intake."( Pharmacokinetics of rokitamycin after single administration to healthy volunteers.
Benvenuti, C; Bottà, V; Broggini, M; Congedo, M; Fonio, W; Parini, J,
)
1.37
" We measured, using the GA-test, variations in gastric acidities of 43 children with ages between 1 to 14 years, and investigated the relationship between gastric acidities and pharmacokinetic values."( [Microbiological, pharmacokinetic and clinical studies of rokitamycin dry syrup in the pediatric field].
Aramaki, M; Fujimoto, T; Kawakami, A; Koga, T; Motohiro, T; Oda, K; Sakata, Y; Suzuki, K; Tanaka, K; Yamashita, F, 1988
)
0.52
" Pharmacokinetic observations seemed to indicate that RKM achieved higher blood concentrations than older macrolides, but a large individual variation was observed."( [Clinical and pharmacokinetic studies of rokitamycin in children].
Abe, T; Adachi, H; Arimasu, O; Fujii, R; Kakuta, O; Meguro, H; Shinozaki, T; Shiraishi, H; Sugie, N, 1988
)
0.54
"Bacteriological, pharmacokinetic and clinical studies were done on the effect of rokitamycin (RKM, TMS-19-Q) in the field of pediatrics."( [Bacteriological, pharmacokinetic and clinical studies on a rokitamycin dry syrup in the pediatric field].
Hori, M; Joh, K; Sugita, M; Takahashi, T; Toyonaga, Y; Watanabe, Y, 1988
)
0.74

Bioavailability

ExcerptReferenceRelevance
"The absorption and excretion of rokitamycin (RKM) in dry syrup form for children were studied following oral administration to fasted healthy volunteers with high gastric acidity as a suitable model to estimate bioavailability of RKM in children."( [Studies on absorption and excretion of rokitamycin dry syrup in healthy volunteers].
Endo, S; Ishioka, T; Morishita, M; Ohta, K; Sakai, A; Suzuki, T; Yasuda, N, 1988
)
0.83
" After pre-administration of erythromycin the relative bioavailability of nifedipine after oral administration was increased compared with injection into the peritoneal cavity."( Inhibition of nifedipine metabolism in dogs by erythromycin: difference between the gut wall and the liver.
Arimori, K; Nakamura, K; Nakano, M; Tsuruta, S, 1997
)
0.3

Dosage Studied

The results of the study show that treatment with rokitamycin in the short term, at the usual dosage of 800 mg/day, is a valid therapeutic scheme in infective processes in odontostomatology. They also indicated that, as the PAEs of roKitamycin on the M phenotype and inducible resistant strains were comparable with those on susceptible strains, no re-evaluation of therapeutic dosing regimens was required.

ExcerptRelevanceReference
" Daily dosage of 600 mg of rokitamycin was administered orally in three divided doses for 5 days."( [A clinical experience of rokitamycin on Campylobacter enteritis. Research Group of Rokitamycin on Infectious Enteritis].
Irimajiri, S; Nakamura, Y; Nitta, Y; Ota, S; Sagara, H; Sato, J; Seo, T; Takizawa, Y; Tomizawa, I; Tsunoda, T, 1991
)
0.88
" In higher dosage groups (180 and 360 mg/kg), vomiting, salivation and reduction of body weight gain with decrease in food intake were observed."( [Chronic toxicity and recovery tests of rokitamycin in beagle dogs].
Nagata, R; Nagata, T; Onishi, M; Sato, M, 1987
)
0.54
" Results of urinalysis, hematological analysis and biochemical analysis of serum and organ weights were normal except that a dose-dependent hypertrophy of caecum was observed in all dosage groups."( [Comparative toxicity study of rokitamycin and josamycin in rats].
Endo, H; Hayano, K; Matsumoto, K; Miura, M; Morino, T; Shiraiwa, K, 1987
)
0.56
" The study was made by the double-blind controlled trial at the dosage of daily 600 mg in TMS group and 1,200 mg in MDM group."( [Clinical evaluation of the TMS-19-Q.GC tablet on superficial suppurative disease. A comparative double blind study with midecamycin].
Fujita, K; Kukita, A; Miura, Y; Nonami, E; Shigeno, Y; Shishiba, T; Tagami, H; Tanita, Y; Tsukinaga, I; Watanabe, S, 1985
)
0.27
"GC tablet (TMS) with josamycin tablet (JM) in acute tonsillitis, the double blind trial was carried out with the daily dosage of 200 mg X 3 in TMS and 400 mg X 3 in JM."( [Clinical evaluation of the TMS-19-Q.GC tablet in acute tonsillitis. A comparative double blind study with josamycin].
Baba, S; Fujimaki, Y; Kawabata, I; Kawamura, S; Kinoshita, H; Mori, Y; Nomura, Y; Sanbe, B; Sugita, R; Ueda, R, 1985
)
0.27
"GC tablet (TMS), a new macrolide antibiotic preparation, were compared with those of josamycin (JM) in the treatment of acute odontogenic infection under multicentered double-blind controlled study at the daily dosage of 600 mg of TMS or 1,200 mg of JM."( [Clinical evaluation of the TMS-19-Q.GC tablet in odontogenic infections. A comparative double-blind study with josamycin].
Abe, H; Ikeshima, K; Kaneko, A; Mishina, M; Morihana, K; Ohmura, H; Sasaki, J; Sesimo, Y; Takai, H; Yamada, Y, 1985
)
0.27
" The tolerance of rokitamycine (RKM), a new macrolide with a wide activity spectrum in 133 antibiotic-intolerant patients has been studied by open oral challenge with incremental dosage until a cumulative dose of 406 mg."( [Rokitamycin tolerance in patients with adverse reactions to chemotherapeutic agents].
Berteramo, R; Cenci, L; Ferrannini, A; Nettis, E, 1996
)
1.54
" The experiments were of randomized cross-over design with a two-week wash-out period between dosing regimens."( Inhibition of nifedipine metabolism in dogs by erythromycin: difference between the gut wall and the liver.
Arimori, K; Nakamura, K; Nakano, M; Tsuruta, S, 1997
)
0.3
" A controlled clinical study is carried out, in parallel groups, whose aim was to assess the therapeutic action and safety of two dosage schemes of rokitamycin, in the short term treatment (5 days) of acute infective processes of odontostomatological origin."( [Rokitamycin in odontostomatology. Controlled study of doses].
Carbone, V; Fornaseri, C; Giangrandi, D; Giordano, M; Mortellaro, C, 1997
)
1.41
"The results of the study show that treatment with rokitamycin in the short term, at the usual dosage of 800 mg/day, is a valid therapeutic scheme in infective processes in odontostomatology."( [Rokitamycin in odontostomatology. Controlled study of doses].
Carbone, V; Fornaseri, C; Giangrandi, D; Giordano, M; Mortellaro, C, 1997
)
1.46
" They also indicated that, as the PAEs of rokitamycin on the M phenotype and inducible resistant strains were comparable with those on susceptible strains, no re-evaluation of therapeutic dosing regimens was required."( The post-antibiotic effects of rokitamycin (a 16-membered ring macrolide) on susceptible and erythromycin-resistant strains of Streptococcus pyogenes.
Braga, PC; Culici, M; Dal Sasso, M, 2004
)
0.87
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
organic molecular entityAny 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]

Bioassays (38)

Assay IDTitleYearJournalArticle
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID422942Antimicrobial activity against macrolide-susceptible Mycoplasma pneumoniae isolated from pediatric patients with community-acquired pneumonia after 10 to 14 days by microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Increased macrolide resistance of Mycoplasma pneumoniae in pediatric patients with community-acquired pneumonia.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID422944Antimicrobial activity against macrolide-resistant Mycoplasma pneumoniae harboring A2064G transition in domain V of 23S rRNA isolated from pediatric patients with community-acquired pneumonia after 10 to 14 days by microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Increased macrolide resistance of Mycoplasma pneumoniae in pediatric patients with community-acquired pneumonia.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID475092Antibacterial activity against Streptococcus pneumoniae DP1 type 1 after 20 hrs by agar dilution method2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Novel azalides derived from 16-membered macrolides. III. Azalides modified at the C-15 and 4'' positions: Improved antibacterial activities.
AID475102Antibacterial activity against Streptococcus pyogenes 3 expressing mefA efflux pump after 20 hrs by agar dilution method2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Novel azalides derived from 16-membered macrolides. III. Azalides modified at the C-15 and 4'' positions: Improved antibacterial activities.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID475100Antibacterial activity against Streptococcus pyogenes Cook after 20 hrs by agar dilution method2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Novel azalides derived from 16-membered macrolides. III. Azalides modified at the C-15 and 4'' positions: Improved antibacterial activities.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID475101Antibacterial activity against Streptococcus pyogenes 2 expressing constitutive ermB methylase after 20 hrs by agar dilution method2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Novel azalides derived from 16-membered macrolides. III. Azalides modified at the C-15 and 4'' positions: Improved antibacterial activities.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID475094Antibacterial activity against Streptococcus pneumoniae 6 expressing constitutive ermB methylase and mefA after 20 hrs by agar dilution method2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Novel azalides derived from 16-membered macrolides. III. Azalides modified at the C-15 and 4'' positions: Improved antibacterial activities.
AID475095Antibacterial activity against Streptococcus pneumoniae 7 expressing constitutive ermB methylase after 20 hrs by agar dilution method2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Novel azalides derived from 16-membered macrolides. III. Azalides modified at the C-15 and 4'' positions: Improved antibacterial activities.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID475105Antibacterial activity against Haemophilus influenzae 3 after 20 hrs by agar dilution method2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Novel azalides derived from 16-membered macrolides. III. Azalides modified at the C-15 and 4'' positions: Improved antibacterial activities.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID475093Antibacterial activity against Streptococcus pneumoniae 5 expressing constitutive ermB methylase after 20 hrs by agar dilution method2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Novel azalides derived from 16-membered macrolides. III. Azalides modified at the C-15 and 4'' positions: Improved antibacterial activities.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID422943Antimicrobial activity against macrolide-resistant Mycoplasma pneumoniae harboring A2063G transition in domain V of 23S rRNA isolated from pediatric patients with community-acquired pneumonia after 10 to 14 days by microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Increased macrolide resistance of Mycoplasma pneumoniae in pediatric patients with community-acquired pneumonia.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID475103Antibacterial activity against Haemophilus influenzae 1 after 20 hrs by agar dilution method2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Novel azalides derived from 16-membered macrolides. III. Azalides modified at the C-15 and 4'' positions: Improved antibacterial activities.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID475091Antibacterial activity against Staphylococcus aureus 209P JC1 after 20 hrs by agar dilution method2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Novel azalides derived from 16-membered macrolides. III. Azalides modified at the C-15 and 4'' positions: Improved antibacterial activities.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID475099Antibacterial activity against Streptococcus pneumoniae 11 expressing mefA efflux pump after 20 hrs by agar dilution method2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Novel azalides derived from 16-membered macrolides. III. Azalides modified at the C-15 and 4'' positions: Improved antibacterial activities.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID475097Antibacterial activity against Streptococcus pneumoniae 9 expressing inducible ermB methylase after 20 hrs by agar dilution method2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Novel azalides derived from 16-membered macrolides. III. Azalides modified at the C-15 and 4'' positions: Improved antibacterial activities.
AID475096Antibacterial activity against Streptococcus pneumoniae 8 expressing inducible ermB methylase after 20 hrs by agar dilution method2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Novel azalides derived from 16-membered macrolides. III. Azalides modified at the C-15 and 4'' positions: Improved antibacterial activities.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID475098Antibacterial activity against Streptococcus pneumoniae 10 expressing mefA efflux pump after 20 hrs by agar dilution method2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Novel azalides derived from 16-membered macrolides. III. Azalides modified at the C-15 and 4'' positions: Improved antibacterial activities.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID475104Antibacterial activity against Haemophilus influenzae 2 after 20 hrs by agar dilution method2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Novel azalides derived from 16-membered macrolides. III. Azalides modified at the C-15 and 4'' positions: Improved antibacterial activities.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (130)

TimeframeStudies, This Drug (%)All Drugs %
pre-199057 (43.85)18.7374
1990's45 (34.62)18.2507
2000's25 (19.23)29.6817
2010's2 (1.54)24.3611
2020's1 (0.77)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 22.37

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 Index22.37 (24.57)
Research Supply Index5.05 (2.92)
Research Growth Index4.08 (4.65)
Search Engine Demand Index26.67 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.37)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials16 (11.51%)5.53%
Reviews3 (2.16%)6.00%
Case Studies4 (2.88%)4.05%
Observational0 (0.00%)0.25%
Other116 (83.45%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]