Page last updated: 2024-12-06

squalamine

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

Description

Squalamine is a naturally occurring aminosteroid that was first isolated from the shark’s liver. It has been shown to have a wide range of biological activities, including anti-cancer, anti-viral, and anti-inflammatory properties. Squalamine's ability to inhibit angiogenesis, the formation of new blood vessels, makes it a promising target for the treatment of cancer and other diseases. Squalamine is also being investigated for its potential to treat Alzheimer’s disease and other neurodegenerative disorders. However, despite promising preclinical studies, squalamine has not yet been approved for human use.'

squalamine: from dogfish shark Squalus acanthias; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID72495
CHEMBL ID444929
CHEBI ID80765
SCHEMBL ID12836
MeSH IDM0213175

Synonyms (29)

Synonym
squalamine
148717-90-2
(3beta,5alpha,7alpha,24r)-3-((3-(4-(aminobutyl)amino)propyl)amio)cholestane-7,24-diol 24-(hydrogen sulfate)
3beta-n-1-(n-(3-(4-aminobutyl))-1,3-diaminopropane)-7alpha,24-dihydroxy-5alpha-cholestane 24-sulfate
squalamine [inn]
3-((3-(4-(aminobutyl)amino)propyl)amio)cholestane-7,24-diol 24-(hydrogen sulfate), (3beta,5alpha,7alpha,24r)-
cholestane-7,24-diol, 3-((3-(4-(aminobutyl)amino)propyl)amio)-, 24-(hydrogen sulfate), (3beta,5alpha,7alpha,24r)-
[(3r,6r)-6-[(3s,5r,7r,8r,9s,10s,13r,14s,17r)-3-[3-(4-aminobutylamino)propylamino]-7-hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylheptan-3-yl] hydrogen sulfate
CHEMBL444929
chebi:80765 ,
f8po54z4v7 ,
unii-f8po54z4v7
squalamine [who-dd]
squalamine [mi]
3beta-n-1-(n-[3-(4-aminobutyl)]- 1,3-diaminopropane)-7alpha,24r-dihydroxy-5alpha-cholestane 24-sulfate
LMST05050024
SCHEMBL12836
HY-16468
AKOS030526099
DTXSID40869971
DB06461
msi-1256
UIRKNQLZZXALBI-MSVGPLKSSA-N
Q15427852
msi-1256f (squalamine lactate)
gtpl10861
7alpha-hydroxy, 3beta-spermidine
F85142
MS-30835

Research Excerpts

Overview

Squalamine is a novel aminosterol recently isolated from the dogfish shark, Squalus acanthias. Squalamine mimics are a new class of broad-spectrum antimicrobial agents.

ExcerptReferenceRelevance
"Squalamine is a steroid extracted from sharks with proven in vitro antibacterial activity. "( Antibacterial efficacy of inhaled squalamine in a rat model of chronic Pseudomonas aeruginosa pneumonia.
Andrieu, V; Brégeon, F; Brunel, JM; Hraiech, S; Lepidi, H; Papazian, L; Raoult, D; Roch, A; Rolain, JM, 2012
)
2.1
"Squalamine is an antitumor agent that has been shown to have antiangiogenic activity in animal models. "( A phase I/IIA trial of continuous five-day infusion of squalamine lactate (MSI-1256F) plus carboplatin and paclitaxel in patients with advanced non-small cell lung cancer.
Allgood, V; Bekele, BN; Carbone, DP; Desai, A; Hait, H; Hammond, LA; Herbst, RS; Holroyd, KJ; Schiller, JH; Solomon, S; Tran, HT; Williams, JI, 2003
)
2.01
"Squalamine is a very active inhibitor of OIR in mouse neonates at doses as low as 1 mg/kg given once."( Regression of retinopathy by squalamine in a mouse model.
Geng, Y; Higgins, RD; Williams, JI; Yan, Y; Zasloff, M, 2004
)
1.34
"Squalamine is a novel aminosterol recently isolated from the dogfish shark, Squalus acanthias. "( Structure of the novel steroidal antibiotic squalamine determined by two-dimensional NMR spectroscopy.
Durell, S; Moore, KS; Roder, H; Wehrli, SL; Zasloff, M, 1993
)
1.99
"Squalamine is a cationic steroid characterized by a condensation of an anionic bile salt intermediate with spermidine."( Squalamine: an aminosterol antibiotic from the shark.
Forrest, JN; McCrimmon, D; Moore, KS; Roder, H; Rogers, M; Wehrli, S; Zasloff, M, 1993
)
2.45
"Squalamine mimics are a new class of broad-spectrum antimicrobial agents."( Antimicrobial activities of squalamine mimics.
Armstrong, D; Bernard, EM; Kikuchi, K; Regen, SL; Sadownik, A, 1997
)
1.31
"Squalamine is a novel cationic steroid that possesses potent, broad spectrum, antimicrobial activity. "( Expression of the K54 and O4 specific antigen has opposite effects on the bactericidal activity of squalamine against an extraintestinal isolate of Escherichia coli.
Mylotte, D; Russo, TA, 1998
)
1.96
"Squalamine is a novel anti-angiogenic aminosterol that is postulated to inhibit neovascularization by selectively inhibiting the sodium-hydrogen antiporter exchanger. "( Potentiation of platinum antitumor effects in human lung tumor xenografts by the angiogenesis inhibitor squalamine: effects on tumor neovascularization.
Bittner, G; Schiller, JH, 1999
)
1.96
"Squalamine is a natural antiangiogenic sterol, and its potential role in treatment of ovarian cancers with or without standard cisplatin chemotherapy was assessed."( Squalamine and cisplatin block angiogenesis and growth of human ovarian cancer cells with or without HER-2 gene overexpression.
Li, D; Pietras, RJ; Williams, JI, 2002
)
2.48

Effects

ExcerptReferenceRelevance
"Squalamine has no observable effect on unstimulated endothelial cells, is not directly cytotoxic to tumor cells, does not alter mitogen production by tumor cells, and has no obvious effects on the growth of newborn vertebrates."( Squalamine inhibits angiogenesis and solid tumor growth in vivo and perturbs embryonic vasculature.
Brem, H; Chao, TL; Cheshire, K; Davis, JD; Donowitz, M; Epstein, DS; Gannon, FH; Kinney, WA; Laterra, J; McLane, MP; Pitchford, S; Sills, AK; Sipos, EP; Tyler, BM; Williams, JI; Zasloff, M, 1998
)
2.46

Actions

ExcerptReferenceRelevance
"The squalamine mimics, because of their potencies, broad spectra of antimicrobial activity, and potential for systemic toxicity, appear to be good candidates for development as topical antimicrobial agents."( Antimicrobial activities of squalamine mimics.
Armstrong, D; Bernard, EM; Kikuchi, K; Regen, SL; Sadownik, A, 1997
)
1.07

Treatment

Squalamine (1-h pretreatment) decreased the maximal velocity of rabbit NHE3 in a concentration-dependent manner. Squalamine treatment was found to retard two cellular events necessary for angiogenesis.

ExcerptReferenceRelevance
"Squalamine (1-h pretreatment) decreased the maximal velocity of rabbit NHE3 in a concentration-dependent manner (13, 47, and 57% inhibition with 3, 5, and 7 micrograms/ml, respectively) and also increased K'[H+]i."( Squalamine, a novel cationic steroid, specifically inhibits the brush-border Na+/H+ exchanger isoform NHE3.
Akhter, S; Donowitz, M; Nath, SK; Tse, CM; Williams, J; Zasloff, M, 1999
)
2.47
"Squalamine treatment was found to retard two cellular events necessary for angiogenesis, inducing disorganization of F-actin stress fibers and causing a concomitant reduction of detectable cell the surface molecular endothelial cadherin (VE-cadherin)."( Squalamine treatment of human tumors in nu/nu mice enhances platinum-based chemotherapies.
Chen, Q; Gonzalez, CM; Holroyd, KJ; Jundt, CH; Marty, J; Mclane, MP; Stringer, SD; Von Hoff, DD; Weitman, S; Williams, JI; Zasloff, M, 2001
)
2.47

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic calculations revealed a linear relationship between area under the curve or Cmax and squalamine dose rate up to 384 mg/m(2)/day, with a prolonged terminal squalamine persistence in patient plasma (median t(1/2) = 18 h; range, 8-48 h)."( A phase I and pharmacokinetic study of squalamine, a novel antiangiogenic agent, in patients with advanced cancers.
Bhargava, P; Dahut, W; Hait, H; Hawkins, MJ; Holroyd, KJ; Marshall, JL; Rizvi, N; Song, S; Trocky, N; Williams, JI, 2001
)
0.8
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35

Dosage Studied

ExcerptRelevanceReference
" At high phospholipid concentrations, the leakage of CF from PC LUVs deviates from a simple dose-response relationship, and it appears that some of the squalamine can no longer cause leakage."( The aminosterol antibiotic squalamine permeabilizes large unilamellar phospholipid vesicles.
Dollahon, NR; Fojtik, KG; Jones, SR; Selinsky, BS; Shinnar, AE; Zhou, Z, 1998
)
0.8
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
bile acidAny member of a group of hydroxy-5beta-cholanic acids occuring in bile, where they are present as the sodium salts of their amides with glycine or taurine. In mammals bile acids almost invariably have 5beta-configuration.
[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 (79)

Assay IDTitleYearJournalArticle
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]
AID1578866Potentiation of chloramphenicol-induced antibacterial activity against Enterobacter aerogenes ATCC 13048 assessed as chloramphenicol MIC at 1.6 ug/ml after 18 hrs (Rvb = 4 ug/ml)2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Antibiotic Adjuvants: Make Antibiotics Great Again!
AID1578865Potentiation of ciprofloxacin-induced antibacterial activity against Enterobacter aerogenes ATCC 13048 assessed as ciprofloxacin MIC at 1.6 ug/ml after 18 hrs (Rvb = 0.5 ug/ml)2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Antibiotic Adjuvants: Make Antibiotics Great Again!
AID1578864Potentiation of erythromycin-induced antibacterial activity against Pseudomonas aeruginosa PAO1 assessed as erythromycin MIC at 3.2 ug/ml after 18 hrs (Rvb = 512 ug/ml)2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Antibiotic Adjuvants: Make Antibiotics Great Again!
AID380055Antimicrobial activity against Candida albicans ATCC 900282000Journal of natural products, May, Volume: 63, Issue:5
Aminosterols from the dogfish shark Squalus acanthias.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID206366Evaluated for its in vitro antimicrobial activity against Staphylococcus equisimilis (6580C)2001Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
Synthesis and antimicrobial activity of new 3 alpha-hydroxy-23,24-bisnorcholane polyamine carbamates.
AID205962Evaluated for its in vitro antimicrobial activity against Staphylococcus aureus (6538p)2001Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
Synthesis and antimicrobial activity of new 3 alpha-hydroxy-23,24-bisnorcholane polyamine carbamates.
AID622482Antibacterial activity against Staphylococcus aureus assessed as induction of bacterial membrane depolarization at MIC after 3 mins by fluorescence assay2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial activities.
AID1254478Antibacterial activity against Escherichia coli ATCC 25922 after 24 hrs by broth microdilution method2015Bioorganic & medicinal chemistry, Dec-01, Volume: 23, Issue:23
Helical peptide-polyamine and -polyether conjugates as synthetic ionophores.
AID380052Antimicrobial activity against Staphylococcus aureus ATCC 292182000Journal of natural products, May, Volume: 63, Issue:5
Aminosterols from the dogfish shark Squalus acanthias.
AID622389Antibacterial activity against colistin-sensitive Pseudomonas aeruginosa after 24 hrs by microbroth dilution method2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial 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]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID228754In vitro minimal hemolytic activity was determined;ND means not done.2001Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
Synthesis and antimicrobial activity of new 3 alpha-hydroxy-23,24-bisnorcholane polyamine carbamates.
AID1254477Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 after 24 hrs by broth microdilution method2015Bioorganic & medicinal chemistry, Dec-01, Volume: 23, Issue:23
Helical peptide-polyamine and -polyether conjugates as synthetic ionophores.
AID622385Antibacterial activity against oxacillin-sensitive Staphylococcus aureus after 24 hrs by microbroth dilution method2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial activities.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID622395Antibacterial activity against Staphylococcus aureus ATCC 25923 after 24 hrs by microbroth dilution method in presence of Mg2+2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial activities.
AID70734Evaluated for its antimicrobial activity against Escherichia coli (25922)2001Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
Synthesis and antimicrobial activity of new 3 alpha-hydroxy-23,24-bisnorcholane polyamine carbamates.
AID1254474Antifungal activity against Candida albicans clinical isolate after 48 hrs by broth microdilution method2015Bioorganic & medicinal chemistry, Dec-01, Volume: 23, Issue:23
Helical peptide-polyamine and -polyether conjugates as synthetic ionophores.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID622396Ratio of MIC for Escherichia coli ATCC 25922 in presence of Mg2+ to MIC for Escherichia coli ATCC 25922 in absence of Mg2+2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial activities.
AID1578869Potentiation of erythromycin-induced antibacterial activity against Enterobacter aerogenes ATCC 13048 assessed as erythromycin MIC at 1.6 ug/ml after 18 hrs (Rvb = 512 ug/ml)2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Antibiotic Adjuvants: Make Antibiotics Great Again!
AID622386Antibacterial activity against oxacillin-resistant Staphylococcus aureus after 24 hrs by microbroth dilution method2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial activities.
AID1578862Potentiation of tetracycline-induced antibacterial activity against Pseudomonas aeruginosa PAO1 assessed as tetracycline MIC at 3.2 ug/ml after 18 hrs (Rvb = 16 ug/ml)2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Antibiotic Adjuvants: Make Antibiotics Great Again!
AID622481Antibacterial activity against Staphylococcus aureus assessed as induction of bacterial membrane depolarization at MIC measured up to 21 mins by fluorescence assay2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial activities.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID622384Antibacterial activity against Staphylococcus aureus after 24 hrs by microbroth dilution method2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial activities.
AID1578860Potentiation of chloramphenicol-induced antibacterial activity against Pseudomonas aeruginosa PAO1 assessed as chloramphenicol MIC at 3.2 ug/ml after 18 hrs (Rvb = 512 ug/ml)2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Antibiotic Adjuvants: Make Antibiotics Great Again!
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1578859Potentiation of erythromycin-induced antibacterial activity against Escherichia coli AG100 assessed as erythromycin MIC at 0.4 ug/ml after 18 hrs (Rvb = 512 ug/ml)2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Antibiotic Adjuvants: Make Antibiotics Great Again!
AID622479Antibacterial activity against Staphylococcus aureus assessed as induction of ATP efflux at 4 times MIC after 5 mins by luminometry2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial 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
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1578856Potentiation of ciprofloxacin-induced antibacterial activity against Escherichia coli AG100 assessed as ciprofloxacin MIC at 0.4 ug/ml after 18 hrs (Rvb = 0.25 ug/ml)2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Antibiotic Adjuvants: Make Antibiotics Great Again!
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1578857Potentiation of tetracycline-induced antibacterial activity against Escherichia coli AG100 assessed as tetracycline MIC at 0.4 ug/ml after 18 hrs (Rvb = 2 ug/ml)2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Antibiotic Adjuvants: Make Antibiotics Great Again!
AID1578863Potentiation of cefepime-induced antibacterial activity against Pseudomonas aeruginosa PAO1 assessed as cefepime MIC at 3.2 ug/ml after 18 hrs (Rvb = 8 ug/ml)2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Antibiotic Adjuvants: Make Antibiotics Great Again!
AID1542776Induction of membrane depolarization in Staphylococcus aureus ATCC 25923 measured after 15 mins by DiSC3(5) dye based spectrofluorometric method2019Bioorganic & medicinal chemistry, 05-15, Volume: 27, Issue:10
6-Bromoindolglyoxylamido derivatives as antimicrobial agents and antibiotic enhancers.
AID622480Antibacterial activity against Escherichia coli assessed as induction of bacterial membrane depolarization at MIC measured up to 21 mins by fluorescence assay2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial activities.
AID622393Antibacterial activity against Staphylococcus aureus ATCC 25923 after 24 hrs by microbroth dilution method in absence of Mg2+2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial activities.
AID96237Evaluated for its antimicrobial activity against Klebsiella pneumoniae (10031)2001Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
Synthesis and antimicrobial activity of new 3 alpha-hydroxy-23,24-bisnorcholane polyamine carbamates.
AID1578855Potentiation of chloramphenicol-induced antibacterial activity against Escherichia coli AG100 assessed as chloramphenicol MIC at 0.4 ug/ml after 18 hrs (Rvb = 8 ug/ml)2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Antibiotic Adjuvants: Make Antibiotics Great Again!
AID1254476Antibacterial activity against Staphylococcus aureus 34 clinical isolate after 24 hrs by broth microdilution method2015Bioorganic & medicinal chemistry, Dec-01, Volume: 23, Issue:23
Helical peptide-polyamine and -polyether conjugates as synthetic ionophores.
AID200863Evaluated for its antimicrobial activity against Salmonella Typhimurium (14028)2001Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
Synthesis and antimicrobial activity of new 3 alpha-hydroxy-23,24-bisnorcholane polyamine carbamates.
AID245335Minimal inhibitory concentration against Staphylococcus aureus (strain CIP 54127) after 48 hr of incubation was evaluated2004Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16
Synthesis of 7 alpha- and 7 beta-spermidinylcholesterol, squalamine analogues.
AID1578861Potentiation of ciprofloxacin-induced antibacterial activity against Pseudomonas aeruginosa PAO1 assessed as ciprofloxacin MIC at 3.2 ug/ml after 18 hrs (Rvb = 16 ug/ml)2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Antibiotic Adjuvants: Make Antibiotics Great Again!
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]
AID622477Antibacterial activity against Escherichia coli assessed as induction of ATP efflux at 4 times MIC after 5 mins by luminometry analysis2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial 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]
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]
AID164872Evaluated for its antimicrobial activity against Pseudomonas aeruginosa (27853)2001Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
Synthesis and antimicrobial activity of new 3 alpha-hydroxy-23,24-bisnorcholane polyamine carbamates.
AID622390Antibacterial activity against colistin-resistant Inquilinus limosus after 24 hrs by microbroth dilution method2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial activities.
AID622388Antibacterial activity against Pseudomonas aeruginosa after 24 hrs by microbroth dilution method2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial activities.
AID40187Evaluated for its in vitro antimicrobial activity against Bacillus subtilis (6633)2001Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
Synthesis and antimicrobial activity of new 3 alpha-hydroxy-23,24-bisnorcholane polyamine carbamates.
AID245241Minimal inhibitory concentration against Escherichia coli (strain 54127) after 48 hr of incubation was evaluated2004Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16
Synthesis of 7 alpha- and 7 beta-spermidinylcholesterol, squalamine analogues.
AID1578858Potentiation of cefepime-induced antibacterial activity against Escherichia coli AG100 assessed as cefepime MIC at 0.4 ug/ml after 18 hrs (Rvb = 0.5 ug/ml)2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Antibiotic Adjuvants: Make Antibiotics Great Again!
AID123055Evaluated for its antimicrobial activity against Micrococcus luteus (9341)2001Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
Synthesis and antimicrobial activity of new 3 alpha-hydroxy-23,24-bisnorcholane polyamine carbamates.
AID380053Antimicrobial activity against Escherichia coli ATCC 259222000Journal of natural products, May, Volume: 63, Issue:5
Aminosterols from the dogfish shark Squalus acanthias.
AID622387Antibacterial activity against Escherichia coli after 24 hrs by microbroth dilution method2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial activities.
AID162745Evaluated for its antimicrobial activity against Proteus mirabilis (25933)2001Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
Synthesis and antimicrobial activity of new 3 alpha-hydroxy-23,24-bisnorcholane polyamine carbamates.
AID622391Antibacterial activity against Colistin resistant Burkholderia cepacia after 24 hrs by microbroth dilution method2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial activities.
AID205395Evaluated for its antimicrobial activity against Serratia marcescens (27117)2001Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
Synthesis and antimicrobial activity of new 3 alpha-hydroxy-23,24-bisnorcholane polyamine carbamates.
AID622392Antibacterial activity against Escherichia coli ATCC 25922 after 24 hrs by microbroth dilution method in absence of Mg2+2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial activities.
AID622394Antibacterial activity against Escherichia coli ATCC 25922 after 24 hrs by microbroth dilution method in presence of Mg2+2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial activities.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID380054Antimicrobial activity against Pseudomonas aeruginosa ATCC 278532000Journal of natural products, May, Volume: 63, Issue:5
Aminosterols from the dogfish shark Squalus acanthias.
AID245475Minimal inhibitory concentration against Candida albicans (strain CIP 1180-79) after 48 hr of incubation was evaluated; Range = 4 - 8 ug/mL2004Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16
Synthesis of 7 alpha- and 7 beta-spermidinylcholesterol, squalamine analogues.
AID1578867Potentiation of tetracycline-induced antibacterial activity against Enterobacter aerogenes ATCC 13048 assessed as tetracycline MIC at 1.6 ug/ml after 18 hrs (Rvb = 2 ug/ml)2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Antibiotic Adjuvants: Make Antibiotics Great Again!
AID1578868Potentiation of cefepime-induced antibacterial activity against Enterobacter aerogenes ATCC 13048 assessed as cefepime MIC at 1.6 ug/ml after 18 hrs (Rvb = 0.25 ug/ml)2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Antibiotic Adjuvants: Make Antibiotics Great Again!
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (83)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's12 (14.46)18.2507
2000's38 (45.78)29.6817
2010's29 (34.94)24.3611
2020's4 (4.82)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 39.87

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.

MetricThis Compound (vs All)
Research Demand Index39.87 (24.57)
Research Supply Index4.52 (2.92)
Research Growth Index4.62 (4.65)
Search Engine Demand Index59.54 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (39.87)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials5 (5.81%)5.53%
Reviews10 (11.63%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other71 (82.56%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (12)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Phase II Study of the Efficacy and Safety of Squalamine Lactate Ophthalmic Formulation 0.2% BID in Subjects With Neovascular AMD. [NCT01678963]Phase 2142 participants (Actual)Interventional2012-11-30Completed
Open Label Squalamine Lactate Ophthalmic Solution for the Treatment of Macular Edema Secondary to Branch Retinal Vein Occlusion (BRVO) and Central Retinal Vein Occlusion (CRVO) [NCT02614937]Phase 1/Phase 220 participants (Actual)Interventional2013-04-30Completed
[NCT00089830]Phase 2120 participants Interventional2004-08-31Terminated
An Open Label Randomized Phase 2 Study To Evaluate The Activity, Tolerability, And Toxicity Of Combined Neoadjuvant Anti-angiogenesis and Androgen Ablation Therapy in Men Undergoing Radical Prostatectomy [NCT00244920]Phase 20 participants (Actual)Interventional2002-01-31Withdrawn(stopped due to Sponsor withdrew drug.)
OHR-1601: A Phase III Study of the Efficacy and Safety of Squalamine Lactate Ophthalmic Solution, 0.2% Twice Daily in Subjects With Neovascular Age-Related Macular Degeneration (AMD) [NCT02727881]Phase 3230 participants (Actual)Interventional2016-04-12Active, not recruiting
"Safety and Efficacy of MSI-1256F (Squalamine Lactate) in Combination With Verteporfin in Patients With Wet Age-Related Macular Degeneration (AMD)" [NCT00094120]Phase 260 participants Interventional2004-10-31Terminated
A Phase 2, Randomized, Open Label, Safety, and Pharmacodynamic Study of Squalamine Lactate for Injection for the Treatment of Minimally Classic or Active Occult Choroidal Neovascularization Associated With Age-Related Macular Degeneration [NCT00333476]Phase 2140 participants Interventional2006-05-31Terminated
A Phase IIA Trial of Continuous Five Day Infusions of MSI-1256F (Squalamine Lactate) Plus Carboplatin for Therapy of Refractory and Resistant Stage III and IV Ovarian Cancer [NCT00021385]Phase 20 participants Interventional2001-05-31Active, not recruiting
A Phase 3, Multicenter, Randomized, Double-Masked, Controlled Study of Squalamine Lactate (MSI-1256F) for Injection for the Treatment of Subfoveal Choroidal Neovascularization Associated With Age-Related Macular Degeneration [NCT00139282]Phase 30 participants Interventional2005-06-30Terminated
A Study of Safety, Functional and Anatomical Effect of Squalamine Lactate Ophthalmic Solution, 0.2% Administered Twice Daily in Subjects With Neovascular Age-related Macular Degeneration [NCT02511613]Phase 20 participants (Actual)Interventional2015-07-31Withdrawn(stopped due to Company decision)
Topical Squalamine in the Treatment of Retinal Neovascularization From Proliferative Diabetic Retinopathy [NCT01769183]Phase 26 participants (Actual)Interventional2013-02-28Completed
A Randomized, Controlled Study of the Safety and Efficacy of Squalamine Lactate Eye Drops in Combination With Ranibizumab in Patients With Diabetic Macular Edema [NCT02349516]Phase 20 participants (Actual)Interventional2015-02-28Withdrawn(stopped due to Study cancelled as of 9/12/15. 0 subjects enrolled.)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]