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Drug

D0015 | Bosentan

Molecular Formula C27H29N5O6S
Molecular Weight 551.6
Structure
State solid
Clearance * 4 L/h [patients with pulmonary arterial hypertension]
Volume of distribution * 18 L
Route of elimination Bosentan is eliminated by biliary excretion following metabolism in the liver.
Protein binding Greater than 98% to plasma proteins, mainly albumin.
Half life Terminal elimination half-life is about 5 hours in healthy adult subjects.
Absorption Absolute bioavailability is approximately 50% and food does not affect absorption.
Description dual endothelin receptor antagonist

C

C02KX01 Bosentan


[C02KX] Antihypertensives for pulmonary arterial hypertension


[C02K] OTHER ANTIHYPERTENSIVES


[C02] ANTIHYPERTENSIVES


[C] Cardiovascular system

Pictogram Signal Statements Precautionary Statement Codes
Danger

Aggregated GHS information provided by 3 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.


H302 (33.33%): Harmful if swallowed [Warning Acute toxicity, oral]


H360 (33.33%): May damage fertility or the unborn child [Danger Reproductive toxicity]


H361 (66.67%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]


H412 (66.67%): Harmful to aquatic life with long lasting effects [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, P264, P270, P273, P281, P301+P312, P308+P313, P330, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)

  • Cardiac failure chronic

  • Connective tissue disorder

  • Heart disease congenital

  • Hepatotoxicity

  • Hypertension

  • Immunodeficiency

  • Lung disorder

  • Pulmonary arterial hypertension

  • Pulmonary hypertension

  • Pulmonary veno-occlusive disease

  • Scleroderma

  • Skin ulcer

  • Systemic sclerosis

  • Ulcer

  • Anaemia (0.08)

  • Wheezing (0.02)

  • Arthralgia

  • Back pain

  • Bladder pain

  • Bronchitis

  • Chest pain

  • Contusion

  • Cough

  • Cystitis

  • Cystitis noninfective

  • Dizziness

  • Dyspnoea

  • Epistaxis

  • Flushing

  • Haemoptysis

  • Headache

  • Hypotension

  • Loss of consciousness

  • Lower respiratory tract infection

  • Muscle spasms

  • Musculoskeletal discomfort

  • Nasal congestion

  • Nasopharyngitis

  • Oedema

  • Orthostatic hypotension

  • Pain in extremity

  • Palpitations

  • Pneumonia

  • Pruritus

  • Pulmonary hypertension

  • Respiratory tract infection

  • Shock

  • Sinusitis

  • Syncope

  • Tracheobronchitis

  • Upper respiratory tract infection

  • Urinary tract infection

  • Vertigo

  • Vision blurred

    • 1196074-08-4 144096-EP2287165A2 144096-EP2287166A2
    144096-EP2292620A2 147536-97-8 174227-18-0
    212B550 4-(1,1-Dimethylethyl)-N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-(2,2''-bipyrimidin)-4-yl) benzenesulfornamide 4-(1,1-Dimethylethyl)-N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-(2,2'-bipyrimidin)-4-yl) benzenesulfornamide
    4-(1,1-Dimethylethyl)-N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-(2,2'-bipyrimidin)-4-yl)benzenesulfornamide 4-(1,1-dimethylethyl)-n-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2'-bipyrimidin]-4-yl]benzenesulfonamide 4-(tert-Butyl)-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2'-bipyrimidin]-4-yl]benzenesulfonamide
    4-(tert-butyl)-N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-[2,2'-bipyrimidin]-4-yl)benzenesulfonamide 4-t-butyl-N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2,2'-bipyrimidin-4-yl)benzenesulfonamide 4-tert butyl-N-[4-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)pyrimidin-6-yl]benzenesulphonamide
    4-tert-Butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-[2,2']bipyrimidinyl-4-yl]-benzenesulfonamide 4-tert-Butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(pyrimidin-2-yl)pyrimidin-4-yl]benzenesulfonamide 4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2,2''-bipyrimidin-4-yl]benzenesulfonamide
    4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2,2'-bipyrimidin-4-yl]benzenesulfonamide 4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyrimidinyl]benzenesulfonamide 4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(pyrimidin-2-yl)pyrimidin-4-yl]benzene-1-sulfonamide
    4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-ylpyrimidin-4-yl]benzenesulfonamide 4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-[2,2'-bipyrimidine]-4-yl]benzene-1-sulfonamide 4-tert-butyl-N-[6-(2-hydroxyethyloxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-yl-pyrimidin-4-yl]benzenesulfonamide
    4-tert-butyl-n-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2,2'-bipyrimidin-4-yl)benzenesulfonamide A808658 AB0018010
    AB01275536-01 ABP001094 AC-148
    ACN-048487 AKOS015852063 AM84442
    Actelion B5118 BCP05202
    BCP9000445 BDBM50061101 Benzenesulfonamide, 4-(1,1-dimethylethyl)-N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)(2,2'-bipyrimidin)-4-yl)-
    Benzenesulfonamide, 4-(1,1-dimethylethyl)-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2'-bipyrimidin]-4-yl]- Bosentan Bosentan (INN)
    Bosentan [USAN:INN:BAN] C27H29N5O6S CAS-147536-97-8
    CCG-221182 CHEBI:51450 CHEMBL957
    CS-0381 CTK4D4929 D07538
    DB00559 DSSTox_CID_26627 DSSTox_GSID_46627
    DSSTox_RID_81776 DTXSID7046627 EN002863
    FT-0658809 GJPICJJJRGTNOD-UHFFFAOYSA-N GTPL3494
    HMS2090N14 HMS3652F15 HMS3715N05
    HMS3750A13 HY-A0013 J-008366
    K86 KS-5062 L001086
    LS-31532 MCULE-3074160312 N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-yl-pyrimidin-4-yl]-4-tert-butyl-benzenesulfonamide
    NCGC00167440-01 NCGC00167440-02 PDSP1_001731
    PDSP2_001714 PubChem19119 Q419769
    Ro 47-0203 Ro 47-0203/039 Ro-47-0203
    Ro-47-0203-029 Ro-47-0203/029 Ro-47-0203/039
    Ro-470203029 SB17356 SC-19679
    SCHEMBL4218 SR-05000001532 SR-05000001532-1
    SR-05000001532-2 SR-05000001532-4 SW199648-3
    Tox21_112444 Tox21_112444_1 Tracleer
    UNII-XUL93R30K2 VA10428 W-5165
    XUL93R30K2 Z1541632805 ZINC1538857
    bosentanum p-tert-Butyl-N-(6-(2-hydroxyethoxy)-5-(o-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyrimidinyl)benzenesulfonamide s4220

    DrugBank Name Bosentan
    DrugBank DB00559
    CAS Number 1065472-77-6, 1174918-31-0, 147536-97-8, 157212-55-0, 174227-18-0
    PubChem Compound 104865
    KEGG Drug D01227/D07538
    PubChem.Substance 46507154
    ChEBI 51450
    PharmGKB PA10034
    ChemSpider 94651
    BindingDB 50061101.0
    TTD DNC000341
    Wikipedia Bosentan
    HET K86
    DPD 12538

    1. Dykens et al. (2007)