Drug

D0944 | fluticasone propionate

Molecular Formula C25H31F3O5S
Molecular Weight 500.6
Structure
State solid
Clearance 1093mL/min for fluticasone propionate[F4358]. A study of 24 healthy Caucasian males showed a clearance of 63.9L/h following intravenous administration[A7490].
Volume of distribution The volume of distribution of intravenous fluticasone propionate is 4.2L/kg[F4358][FDA Label]. A study of 24 healthy Caucasian males showed a volume of distribution at steady state of 577L following intravenous administration[A7490].
Route of elimination Fluticasone propionate is mainly eliminated in the feces with <5% eliminated in the urine[F4358,A176918][FDA Label].
Protein binding Fluticasone propionate is 99% protein bound in serum[F4358]. Topical fluticasone propionate is only 91% protein bound in serum however[F4355].
Half life 7.8 hours for intravenous fluticasone propionate[F4358][FDA Label]. A study of 24 healthy Caucasian males shows a half life of 14.0 hours following intravenous administration and 10.8 hours following inhalation[A7490].
Absorption Intranasal bioavailability of fluticasone propionate is <2%, and oral bioavailability is <1%[F4358][FDA Label]. Intranasal exposure results in the majority of the dose being swallowed[A177118]. Topical absorption of fluticasone propionate is very low but can change depending on a number of factors including integrity of the skin and the presence of inflammation or disease[F4355]. A study of 24 healthy Caucasian males showed an inhaled bioavailability of 9.0%[A7490].

Toxicity Dose Time Species Model Method Action Positive criterion Reference
MEMBRANE POTENTIAL 9.02±1.71 human qHTS-HepG2 MMP assay decrease IC50 163
MEMBRANE POTENTIAL human HepG2 MMP assay Negative IC50 163
MEMBRANE POTENTIAL rat hepatocytes MMP assay Negative IC50 163

Pictogram Signal Statements Precautionary Statement Codes
Danger

Aggregated GHS information provided by 15 companies from 13 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.


Reported as not meeting GHS hazard criteria by 1 of 15 companies. For more detailed information, please visit ECHA C&L website


Of the 12 notification(s) provided by 14 of 15 companies with hazard statement code(s):


H302 (14.29%): Harmful if swallowed [Warning Acute toxicity, oral]


H317 (14.29%): May cause an allergic skin reaction [Warning Sensitization, Skin]


H334 (14.29%): May cause allergy or asthma symptoms or breathing difficulties if inhaled [Danger Sensitization, respiratory]


H360 (42.86%): May damage fertility or the unborn child [Danger Reproductive toxicity]


H361 (50%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]


H373 (64.29%): Causes damage to organs through prolonged or repeated exposure [Warning Specific target organ toxicity, repeated exposure]


H410 (14.29%): Very toxic to aquatic life with long lasting effects [Warning Hazardous to the aquatic environment, long-term hazard]


H413 (14.29%): May cause long lasting harmful effects to aquatic life [Hazardous to the aquatic environment, long-term hazard]


Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.


P201, P202, P260, P261, P264, P270, P272, P273, P280, P281, P285, P301+P312, P302+P352, P304+P341, P308+P313, P314, P321, P330, P333+P313, P342+P311, P363, P391, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)

Organism Test type Route Dose (normalized dose) Effect Source
rat LD50 oral 980mg/kg (980mg/kg) Journal of the American Pharmaceutical Association, Scientific Edition. Vol. 47, Pg. 479, 1958.
cat LDLo intraperitoneal 1gm/kg (1000mg/kg) lungs, thorax, or respiration: other changes Journal of Pharmacology and Experimental Therapeutics. Vol. 101, Pg. 119, 1951.
dog LDLo intraperitoneal 1gm/kg (1000mg/kg) lungs, thorax, or respiration: other changes Journal of Pharmacology and Experimental Therapeutics. Vol. 101, Pg. 119, 1951.
mouse LD50 oral 300mg/kg (300mg/kg) Arzneimittel-Forschung. Drug Research. Vol. 5, Pg. 572, 1955.
rabbit LD50 oral 3200mg/kg (3200mg/kg) Arzneimittel-Forschung. Drug Research. Vol. 5, Pg. 572, 1955.
rabbit LDLo intraperitoneal 1gm/kg (1000mg/kg) lungs, thorax, or respiration: other changes Journal of Pharmacology and Experimental Therapeutics. Vol. 101, Pg. 119, 1951.
cat LDLo oral 150mg/kg (150mg/kg) Arzneimittel-Forschung. Drug Research. Vol. 5, Pg. 572, 1955.
mouse LD50 intravenous 313mg/kg (313mg/kg) behavioral: general anesthetic Journal of Pharmacology and Experimental Therapeutics. Vol. 101, Pg. 119, 1951.
rat LD50 intraperitoneal 600mg/kg (600mg/kg) Journal of Pharmacology and Experimental Therapeutics. Vol. 108, Pg. 450, 1953.
guinea pig LD50 oral 1730mg/kg (1730mg/kg) Journal of the American Pharmaceutical Association, Scientific Edition. Vol. 47, Pg. 479, 1958.
mouse LD50 intraperitoneal 180mg/kg (180mg/kg) Bollettino Chimico Farmaceutico. Vol. 111, Pg. 293, 1972.
guinea pig LDLo intraperitoneal 1gm/kg (1000mg/kg) lungs, thorax, or respiration: other changes Journal of Pharmacology and Experimental Therapeutics. Vol. 101, Pg. 119, 1951.
mouse LD50 subcutaneous 300mg/kg (300mg/kg) Arzneimittel-Forschung. Drug Research. Vol. 8, Pg. 25, 1958.


  • (1R,2S,8S,10S,11S,13R,14R,15S,17S)-1,8-difluoro-14-{[(fluoromethyl)sulfanyl]carbonyl}-17-hydroxy-2,13,15-trimethyl-5-oxotetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-14-yl propanoate (6?,11?,16?,17?)-6,9-Difluoro-11-hydroxy-16-methyl-3-oxo-17-(1-oxopropoxy)androsta-1,4-diene-17-carbothioic acid fluoromethyl ester (6alpha,11beta,16alpha,17alpha)-6,9-Difluoro-11-hydroxy-16-methyl-3-oxo-17-(1-oxopropoxy)androsta-1,4-diene-17-carbothioic acid S-(fluoromethyl) ester
    474F142 6alpha,9-difluoro-17beta-{[(fluoromethyl)sulfanyl]carbonyl}-11beta-hydroxy-16-methyl-3-oxoandrosta-1,4-dien-17alpha-yl propanoate 80474-14-2
    AB00513992 AB00513992-06 AB00513992_08
    AB1010912 AC-457 AKOS015895220
    AN-584/43505443 Androsta-1,4-diene-17-carbothioic acid, 6,9-difluoro-11-hydroxy-16-methyl-3-oxo-17-(1-oxopropoxy)-, (6alpha,11beta,16alpha,17alpha)-S-(fluoromethyl) ester Androsta-1,4-diene-17-carbothioic acid, 6,9-difluoro-11-hydroxy-16-methyl-3-oxo-17-(1-oxopropoxy)-, S-(fluoromethyl) ester, (6-alpha,11-beta,16-alpha,17-alpha)-
    ArmonAir RespiClick ArmonAir RespiClickTM Asmatil
    Axotide BDBM50354849 BIF0710
    BPBio1_001203 BR-72799 BRD-K62310379-001-03-0
    BSPBio_001093 Brethal C25H31F3O5S
    CCG-100981 CCI 18781 CCI-18781
    CHEBI:31441 CHEMBL1473 CS-1986
    Certified Reference Material Cultivate Cutivate
    Cutivate (TN) D01708 DB00588
    FLUTICASONE PROPIONATE FN-25 FT-0082893
    Flixonase Flixonase Nasal Spray Flixotide
    Flixotide Disk Flixotide Disks Flixotide Inhaler
    Flonase Flonase (TN) Flonase Allergy Relief
    Flonase Aq Flovent Flovent (TN)
    Flovent Diskus Flovent Diskus 100 Flovent Diskus 250
    Flovent Diskus 50 Flovent HFA Flovent Rotadisk
    Flovent-hfa Fluinol Flunase
    Flusonal Fluspiral Fluticasone (propionate)
    Fluticasone Impurity B Fluticasone Propionate, Pharmaceutical Secondary Standard Fluticasone propionate (Flonase, Veramyst)
    Fluticasone propionate (JAN/USAN) Fluticasone propionate [USAN:USP] Fluticasone propionate [USAN]
    Fluticasone propionate for impurity C identification, EuropePharmacopoeia (EP) Reference Standard Fluticasone propionate for impurity G identification, EuropePharmacopoeia (EP) Reference Standard; Fluticasone propionate, >=98% (HPLC), powder
    Fluticasone propionate, European Pharmacopoeia (EP) Reference Standard Fluticasone propionate, United States Pharmacopeia (USP) Reference Standard Fluticasonpropionat Allen
    Flutide Flutivate Fluxonal
    GTPL7080 HMS1571G15 HMS2051N19
    HMS2098G15 HMS3413A19 HMS3677A19
    HMS3715G15 HY-B0154 Inalacor
    KS-1173 LS-19323 MFCD00866007
    MLS001424085 NC00231 NCGC00179308-01
    NCGC00179308-05 O2GMZ0LF5W PF-00241939
    Prestwick0_000997 Prestwick1_000997 Prestwick2_000997
    Prestwick3_000997 Q-101393 Q8564098
    Rinosone S-(Fluoromethyl) 6alpha,9-difluoro-11beta,17-dihydroxy-16alpha-methyl-3-oxoandrosta-1,4-diene-17beta-carbothioate, 17-propionate SC-19333
    SCHEMBL4068 SMR000469159 SPBio_002984
    SR-01000763355 SR-01000763355-3 ST2407016
    Skyron Trialona UNII-O2GMZ0LF5W
    Ubizol WMWTYOKRWGGJOA-CENSZEJFSA-N Xhance
    ZINC3920027 Zoflut [(6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-17-(fluoromethylsulfanylcarbonyl)-11-hydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl] propanoate
    atemur s1992

    DrugBank Name fluticasone propionate
    DrugBank DB00588
    CAS Number 65-45-2, 80474-14-2, 90566-53-3, 948566-12-9
    PubChem Compound 444036
    KEGG Drug D01708
    ChEBI 31441
    PharmGKB PA449686