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Drug

D0045 | Efavirenz

Molecular Formula C14H9ClF3NO2
Molecular Weight 315.67
Structure
State solid
Route of elimination Nearly all of the urinary excretion of the radiolabeled drug was in the form of metabolites.
Protein binding 99.5-99.75%
Half life 40-55 hours
Trade names Sustiva, Stocrin
Description non-nucleoside reverse transcriptase inhibitor (NNRTI); antiretroviral agent

J

J05AR11 Lamivudine, tenofovir disoproxil and efavirenz


[J05AR] Antivirals for treatment of HIV infections, combinations


[J05A] DIRECT ACTING ANTIVIRALS


[J05] ANTIVIRALS FOR SYSTEMIC USE


[J] Antiinfectives for systemic use

J05AR06 Emtricitabine, tenofovir disoproxil and efavirenz


[J05AR] Antivirals for treatment of HIV infections, combinations


[J05A] DIRECT ACTING ANTIVIRALS


[J05] ANTIVIRALS FOR SYSTEMIC USE


[J] Antiinfectives for systemic use

J05AG03 Efavirenz


[J05AG] Non-nucleoside reverse transcriptase inhibitors


[J05A] DIRECT ACTING ANTIVIRALS


[J05] ANTIVIRALS FOR SYSTEMIC USE


[J] Antiinfectives for systemic use

Toxicity Dose Time Species Model Method Action Positive criterion Reference
RESPIRATION 197
ROS PRODUCTION increase 197

Pictogram Signal Statements Precautionary Statement Codes
Danger

Aggregated GHS information provided by 87 companies from 11 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.


H302 (51.72%): Harmful if swallowed [Warning Acute toxicity, oral]


H319 (48.28%): Causes serious eye irritation [Warning Serious eye damage/eye irritation]


H360 (48.28%): May damage fertility or the unborn child [Danger Reproductive toxicity]


H372 (42.53%): Causes damage to organs through prolonged or repeated exposure [Danger Specific target organ toxicity, repeated exposure]


H400 (91.95%): Very toxic to aquatic life [Warning Hazardous to the aquatic environment, acute hazard]


H410 (94.25%): Very toxic to aquatic life with long lasting effects [Warning 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, P264, P270, P273, P280, P281, P301+P312, P305+P351+P338, P308+P313, P314, P330, P337+P313, P391, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)

  • Carcinogenicity

  • Dermatitis

  • Drug interaction

  • Foetor hepaticus

  • Hepatitis B

  • Hepatocellular injury

  • HIV infection

  • Immunodeficiency

  • Infection

  • Liver disorder

  • Mental disorder

  • Pathogen resistance

  • Rash

  • Discomfort (0.14)

  • Syncope (0.16)

  • Abdominal pain

  • Abnormal dreams

  • Aggression

  • Anxiety

  • Asthenia

  • Body temperature increased

  • Cough

  • Decreased appetite

  • Depression

  • Dermatitis

  • Dermatitis exfoliative

  • Diarrhoea

  • Disturbance in attention

  • Dizziness

  • Dyspepsia

  • Erythema

  • Erythema multiforme

  • Fatigue

  • Flatulence

  • Gastrointestinal pain

  • Haematuria

  • Headache

  • Hyperhidrosis

  • Hypoaesthesia

  • Insomnia

  • Mental disability

  • Nausea

  • Necrosis

  • Nephrolithiasis

  • Nervousness

  • Pain

  • Pruritus

  • Rash

  • Somnolence

  • Stevens-Johnson syndrome

  • Suicidal ideation

  • Suicide attempt

  • Tension

  • Toxic epidermal necrolysis

  • Vomiting

    • (-)-6-CHLORO-4-CYCLOPROPYLETHYNYL-4-TRIFLUOROMETHYL-1,4-DIHYDRO-2H-3,1-BENZOXAZIN-2-ONE (4S)-6-Chloro-4-(2-cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one (4S)-6-Chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one
    (4S)-6-chloranyl-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-1H-3,1-benzoxazin-2-one (4S)-6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-1H-3,1-benzoxazin-2-one (4S)-6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-2,4-dihydro-1H-3,1-benzoxazin-2-one
    (4S)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-2-one (S)-6-CHLORO-4-(CYCLOPROPYLETHYNYL)-4-(TRIFLUOROMETHYL)-1H-BENZO[D][1,3]OXAZIN-2(4H)-ONE (S)-6-Chloro-4-(cyclopropyl-ethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazine-2-one
    (S)-6-Chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one (S)-6-Chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-benzo[d][1,3]oxazin-2-one (S)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-ben zoxazin-2-one
    (S)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-2-one (S)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2H-benzo[d][1,3]oxazin-2-one (S)-Efavirenz
    (s)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one 154598-52-4 1ikv
    1ikw 2H-3, 6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-, (4S)- 2H-3,1-Benzoxazin-2-one, 6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-, (4S)-
    598E524 6-chloro-4-(2-cyclopropyl-1-ethynyl)-4-trifluoromethyl-(4S)-1,4-dihydro-2H-benzo[d][1,3]oxazin-2-one A809555
    AB00639956-06 AB00639956-08 AB21723
    AC-25006 ACM154801748 AK323634
    AKOS015894951 AOB2950 API0002525
    BCP27719 BCP9000636 BCPP000245
    BDBM2483 BIDD:GT0383 C-19450
    C08088 C14H9ClF3NO2 CAS-154598-52-4
    CC-27439 CCG-101011 CHEBI:119486
    CHEMBL223228 CPD000466351 CS-2154
    CTK8E9137 D00896 DB00625
    DL-535 DMP 266 DMP-266
    DMP-266 DSSTox_CID_26029 DSSTox_GSID_46029
    DSSTox_RID_81298 DTXSID9046029 E0997
    EFV EFV & IFNL1 EFV & IFNL2
    EFV & IFNL3 EFV & IL-28A EFV & IL-28B
    EFV & IL-29 EFV & Interferon lambda-1 EFV & Interferon lambda-2
    EFV & Interferon lambda-3 EFV & Interleukin 28A EFV & Interleukin 28B
    EFV & Interleukin 29 EFV & PLGA Efavirenz
    Efavirenz & IFNL1 Efavirenz & IFNL2 Efavirenz & IFNL3
    Efavirenz & IL-28A Efavirenz & IL-28B Efavirenz & IL-29
    Efavirenz & Interferon lambda-1 Efavirenz & Interferon lambda-2 Efavirenz & Interferon lambda-3
    Efavirenz & Interleukin 28A Efavirenz & Interleukin 28B Efavirenz & Interleukin 29
    Efavirenz & PLGA Efavirenz & Poly-lactide-co-glycolide Efavirenz (JAN/INN)
    Efavirenz [USP:INN:BAN] Efavirenz solution, 1.0 mg/mL in acetonitrile, certified reference material Efavirenz, (S)
    Efavirenz, >=98% (HPLC) Efavirenz, United States Pharmacopeia (USP) Reference Standard Efavirenzum
    Eravirenz FT-0625647 GP6354
    HMS2051J08 HMS2090N16 HMS3393J08
    HMS3713M14 HSDB 7163 HY-10572
    J-520431 JE6H2O27P8 KS-00000ZEH
    KS-00002WWM KS-5380 L 743726
    L-743,726 L-743725 L-743726
    LS-173464 MFCD05662344 MLS000759465
    MLS001424087 Met-SDF-1.beta. & Efavirenz Met-Stromal Cell-derived Factor-1.beta. (Human) & Efavirenz
    NC00261 NCGC00159337-02 NCGC00159337-04
    NCGC00271713-05 NSC-742403 NSC742403
    PubChem5812 Q422645 RTX-012332
    SAM001246667 SC-46515 SCHEMBL37762
    SMR000466351 SR-01000759360 SR-01000759360-4
    SR-01000759360-5 Stocrin Strocin (TM)
    Sustiva Sustiva (TM) Sustiva (TN)
    Tox21_111582 Tox21_111582_1 UNII-JE6H2O27P8
    XPOQHMRABVBWPR-ZDUSSCGKSA-N Z2186909878 ZINC2020233
    efavirenz efavirenz, (S)-isomer s4685

    DrugBank Name Efavirenz
    DrugBank DB00625
    CAS Number 154598-52-4, 154635-17-3, 177530-93-7
    PubChem Compound 64139
    KEGG Compound ID C08088
    KEGG Drug D00896
    PubChem.Substance 46506827
    ChEBI 119486
    PharmGKB PA449441
    ChemSpider 57715
    BindingDB 2483.0
    TTD DAP000709
    Wikipedia Efavirenz
    HET EFZ
    DPD 11857

    1. Vuda et al. (2016)