Etravirine

Các tên gọi khác (1) :

Intelence

reverse transcriptase inhibitors

Thuốc Gốc

Small Molecule

CAS: 269055-15-4

ATC: J05AG04

CTHH: C₂₀H₁₅BrN₆O

PTK: 435.277

Etravirine is an antiretroviral agent more specifically classified as a Non-Nucleoside Reverse Transcriptase Inhibitor(NNRTI). Etraverine is used clinically for the treatment of human immunodeficiency virus type 1 (HIV-1) infection. On January 18, 2007, the FDA granted accelerated approved for the use of etravirine 100mg tablets in the treatment of adult HIV-1 infection documented to be resistant to therapy with other NNRTIs and antiretroviral agents. On March 26, 2012, approval was extended for use in treatment-experienced pediatric patients 6 to 18 years of age, weighing at least 16 kg. Etravarine must always be used in combination with other antiretroviral drugs. Etravirine exerts its effects via direct inhibition of the reverse transcriptase enzyme of human immunodeficiency virus type 1 (HIV-1), and consequently blocks DNA-dependent and RNA-dependent polymerase activity. Etravirine does not inhibit human DNA polymerase alpha, beta or gamma. Common side effects of use include mild to moderate rash within the first 6 weeks of therapy, nausea, diarrhea and peripheral neuropathy. Patients are advised to immediately contact their healthcare provider if a rash develops. In 2009, postmarketing case reports of Stevens-Johnson Syndrome, toxic epidermal necrolysis, erythema multiforme, and other hypersensitivity reactions lead to a revision of etravirine's "Warnings and Precautions," as well as notification of health care providers. In 2013, reports of Autoimmune disorders (such as Graves’ disease, polymyositis, and Guillain-Barré syndrome) in the setting of immune reconstitution, as well as more in depth information about the development of rashes in patients taking etravirine, lead to a modification of etravirine's monograph.

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₂₀H₁₅BrN₆O

Phân tử khối

435.277

Monoisotopic mass

434.049071779

InChI

InChI=1S/C20H15BrN6O/c1-11-7-14(10-23)8-12(2)17(11)28-19-16(21)18(24)26-20(27-19)25-15-5-3-13(9-22)4-6-15/h3-8H,1-2H3,(H3,24,25,26,27)

InChI Key

InChIKey=PYGWGZALEOIKDF-UHFFFAOYSA-N

IUPAC Name

4-({6-amino-5-bromo-2-[(4-cyanophenyl)amino]pyrimidin-4-yl}oxy)-3,5-dimethylbenzonitrile

Traditional IUPAC Name

etravirine

SMILES

CC1=CC(=CC(C)=C1OC1=C(Br)C(N)=NC(NC2=CC=C(C=C2)C#N)=N1)C#N

Độ hòa tan

1.69e-02 g/l

logP

5.54

logS

-4.4

pKa (strongest acidic)

12.49

pKa (Strongest Basic)

4.13

PSA

120.64 Å²

Refractivity

111.87 m³·mol^-1

Polarizability

41.07 Å³

Rotatable Bond Count

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

Ghose Filter

true

Dược Lực Học : Clinical trials have shown no prolongation of QT intervals on electrocardiograms after 8 days of dosing.

Cơ Chế Tác Dụng : Etravirine is an antiretroviral agent more specifically classified as a Non-Nucleoside Reverse Transcriptase Inhibitor(NNRTI). Etraverine is used clinically for the treatment of human immunodeficiency virus type 1 (HIV-1) infection. On January 18, 2007, the FDA granted accelerated approved for the use of etravirine 100mg tablets in the treatment of adult HIV-1 infection documented to be resistant to therapy with other NNRTIs and antiretroviral agents. On March 26, 2012, approval was extended for use in treatment-experienced pediatric patients 6 to 18 years of age, weighing at least 16 kg. Etravarine must always be used in combination with other antiretroviral drugs. Etravirine exerts its effects via direct inhibition of the reverse transcriptase enzyme of human immunodeficiency virus type 1 (HIV-1), and consequently blocks DNA-dependent and RNA-dependent polymerase activity. Etravirine does not inhibit human DNA polymerase alpha, beta or gamma. Common side effects of use include mild to moderate rash within the first 6 weeks of therapy, nausea, diarrhea and peripheral neuropathy. Patients are advised to immediately contact their healthcare provider if a rash develops. In 2009, postmarketing case reports of Stevens-Johnson Syndrome, toxic epidermal necrolysis, erythema multiforme, and other hypersensitivity reactions lead to a revision of etravirine's "Warnings and Precautions," as well as notification of health care providers. In 2013, reports of Autoimmune disorders (such as Graves’ disease, polymyositis, and Guillain-Barré syndrome) in the setting of immune reconstitution, as well as more in depth information about the development of rashes in patients taking etravirine, lead to a modification of etravirine's monograph. Etravirine exerts its effects via direct inhibition of the reverse transcriptase enzyme of human immunodeficiency virus type 1 (HIV-1). It directly binds reverse transcriptase and consequently blocks DNA-dependent and RNA-dependent polymerase activity. Etravirine does not inhibit human DNA polymerase alpha, beta or gamma.

Dược Động Học :

▧ Absorption :
Maximum oral absorption is achieved in 2.5-4 hours. Absorption is unaffected by the concomitant use of oral ranitidine or omeprazole, which decrease gastric acidity. Administration under fasting conditions resulted in a near 50% decrease in systemic exposure (AUC) when compared to administration after a meal.
▧ Volume of Distribution :
Distribution of etravirine into compartments other than plasma has not been evaluated in humans.
▧ Protein binding :
Plasma protein binding is about 99.9% in vitro. In vitro, 99.6% is bound to albumin, and 97.66% - 99.02% is bound to 1-alpha glycoprotein.
▧ Metabolism :
Metabolized (in vitro) by the liver CYP450 enzymes: CYP3A4, CYP2C9, CYP2C19. The major metabolites formed by a methyl hydroxylation of the dimethylbenzonitrile moiety retained less than 90% of etravirine's activity.
▧ Route of Elimination :
After a 800mg dose of radio-labelled etraverine, 93.7% was found to undergo fecal elimination, with 81.2% - 86.4% eliminated unchanged. 1.2% of the dose was renally eliminated, changed. Etravirine is dialyzable (hemodialysis).
▧ Half Life :
Half life of 9.05-41 hours.
▧ Clearance :
Renal clearance of etravirine is negligible (<1.2%), thus no dose adjustments are required in patients with renal impairment. Clearance is shown to be reduced in patients with Hepatitis B and/or co-infection, however, the safety profile of etravirine does not call for dosage adjustments.

Độc Tính :

Chỉ Định : Indicated as an adjunct therapy in the treatment of adult HIV-1 infections resistant to therapy with other NNRTIs and antiretroviral agents.

Tương Tác Thuốc :

Amiodarone Amiodarone, when used concomitantly with etravirine, may decrease in serum concentration. If possible, monitoring for decreased amiodarone levels is recommended.
Amiodarone Amiodarone, when administered concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. If possible, monitoring of amiodarone levels is recommended.
Apixaban Apixaban, when administered concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. Concomitant use should be avoided.
Aripiprazole Ariprazole, when administered concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to increase the dose of oral aripiprazole to maintain therapeutic efficacy, and to adjust the dose of aripiprazole appropriately when the dose of etravirine is altered.
Artemether Artemether, when administered concomitantly with etravirine, may experience a decrease in serum concentrations of active metabolites such as dihydroartemisinin; however, artemether may increase in serum concentration. Etravirine, when used with artemether, may increase in serum concentration. Caution and monitoring of therapeuric efficacy of artemether is recommended.
Atazanavir Atazanavir, when administered concomitantly with etravirine, may experience a decrease in serum concentrations. Etravirine, when administered concomitantly with Atazanavir, may expereince an increase in serum concentrations. Recommended to avoid use of this combination.
Atorvastatin Atorvastatin, when administered concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to monitor continued efficacy of atorvastatin therapy.
Axitinib Axitinib, when administered concomitantly with etravirine, may experience a decrease in serum concentrations. Recommended to avoid use of this combination.
Bepridil Bepridil (withdrawn from US. market), when used concomitantly with etravirine, may experience a decrease in serum concentration. If possible, it is recommended to monitor for decreased bepridil concentrations and therapeutic efficacy.
Boceprevir The exposure of etravirine decreases whereas boceprevir's exposure increased. Therapeutic implications of this observation is unknown.
Bortezomib Bortezombib, when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to avoid this combination.
Bosutinib Bosutinib, when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to avoid this combination.
Brentuximab vedotin Brentuximab, when used concomitantly with etravirine, may experience a decrease in serum concentrations. The levels of an active metabolite of brentuximab, monomethyl auristatin E, may decrease. It is recommended to monitor efficacy of brentuximab therapy.
Buprenorphine Buprenorphine, when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to monitor for a decrease in buprenorphine levels (ie. reduced analgesia, and signs of opioid withdrawal).
Cabozantinib Cabozantinib, when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to avoid this combination if alternative are available. If concurrent use is not avoidable, it is recommended to increase the dosage of cabozantinib by 40mg (without exceeding 180mg/day).
Carbamazepine Carbamazepine, when used concomitantly with certain NNRTIs (ie. efavirenz), may experience a decrease in serum concentration. Etravirine, and other NNRTIs, when used concomitantly with carbamazepine, may experience an increase in serum concentration. It is recommended to avoid this combination.
Carvedilol Carvedilol, when used concomitantly with etravirine (a CYP2C9 inhibitor), may experience an increase in serum concentration. It is recommended to monitor for signs and symptoms of an increased response to carvedilol, such as orthostatic hypotension and bradycardia.
Citalopram Citalopram, when used concomitantly with etravirine (a CYP2C19 inhibitor), may experience an increase in serum concentration. It is recommended to maintain the dose of citalopram below 20mg/day, and to monitor for toxicity. The symptoms which often accompany citalopram overdose are dizziness, sweating, nausea, vomiting, tremor, somnolence,sinus tachycardia,amnesia, confusion, coma, convulsions, hyperventilation, cyanosis, rhabdomyolysis, acute renal failure, and ECG changes (including QTc prolongation, nodal rhythm, ventricular arrhythmia, and torsade de pointes).
Clarithromycin Clarithromycin (and other macrolide antibiotics), when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to use alternative antibiotic agents if available. If concurrent therapy cannot be avoided, monitor for reduced effectiveness of clarithromycin.
Clopidogrel Clopidogrel, when used concomitantly with etravirine (a CYP2C19 inhibitor), may experience a decrease in the serum concentrations of it's active metabolites. Caution and close monitoring for decreased efficacy of clopidogrel is recommended.
Crizotinib Crizotinib, when administered concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid this combination.
Darunavir Etravirine, when used concomitantly with protease inhibitors, may experience a decrease in serum concentration. Protease inhibitors, when used concomitantly with etravirine, may experience an increase in serum concentration. Ritonavir boosting of etravirine therapy is a requirement to concurrent therapy. In addition, it is recommended to monitor serum concentrations of the antiretrovirals, as well as to monitor antiretroviral therapy for efficacy.
Dasatinib Dasatinib, when administered concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid this combination if possible. If concurrent therapy cannot be avoided it is recommended to increase the dose of dasitinib and monitor for efficacy and toxicity.
Deferasirox Etravirine, when administered concomitantly with deferasirox, may experience a decrease in serum concentration. It is recommended to monitor therapy.
Delavirdine Etravirine, when used concomitantly with Delaviridine, may experience an increase in serum concentration. Combination of two NNRTIs has not been demonstrated to be of benefit to HIV therapy. It is recommended to avoid this combination.
Diazepam Diazepam (a CYP21C9 and CYP3A4 substrate), when administered concomitantly with etravirine, may experience an increase (via CYP21C9 inhibition) or a decrease(via CYP3A4 induction) in serum concentration. Overall clinical significance is unknown. It is recommended to monitor diazepam therapy.
Digoxin Digoxin, when administered concomitantly with etravirine, may experience an increase in serum concentration. It is recommended to monitor serum levels of digoxin and titrate dosage to achieve desired therapeutic range. Pre-emptive dose adjustments are not required.
Disopyramide Disopyramide, when administered concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to monitor for disopyramide therapy.
Dronedarone Dronedarone, when administered concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid this combination.
Efavirenz Etravirine, when used concomitantly with Efavirenz, may experience a significant decrease in plasma levels and a loss of efficacy. Combination of two NNRTIs has not been demonstrated to be of benefit to HIV therapy. It is recommended to avoid this combination.
Everolimus Everolimus, when administered concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid this combination. If concurrent therapy cannot be avoided, a gradual dosage increase of everolimus is recommended.
Exemestane Exemestane, when administered concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to increase the dosage of exemestane and to closely monitor therapy for efficacy and toxicity.
Flecainide Flecainide, when administered concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to monitor flecainide therapy.
Fluvastatin Fluvastatin, when administered concomitantly with etravirin, may experience an increase in serum concentration. It is recommended to monitor for signs of toxicity from fluvastatin, such as myopathy and hepatic enzyme elevations.
Fosamprenavir Fosamprenavir, when administered concomitantly with etravirine, may experience an increase in the serum concentration of its active metabolits. It is recommended to avoid this combination.
Fosphenytoin Etravirine, when administered concomitantly with fosphenytoin, may experience a decrease in serum concentration. It is recommended to avoid this combination.
Gefitinib Gefitinib, when administered concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to increase gefitinib dosage, if clinically appropriate, and to monitor for gefitinib therapy for efficacy and toxicity.
Guanfacine Guanfacine, when administered concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to increase guanfacine dosage up to 8mg/day, as tolerated, and to monitor gefitinib therapy.
Ifosfamide Ifosfamide, when administered concomitantly with etravirine (a strong CYP3A4 inducer), may experience an increase in the serum concentrations of its active metabolites. It is recommended to monitor for toxicity of ifosfamide therapy.
Imatinib Imatinib, when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to avoid this combination if alternative are available. If concurrent use is not avoidable, it is recommended to increase the dosage of cabozantinib by a minimum of 50%, and to monitor therapy.
Ivacaftor Ivacaftor, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid this combination.
Ketoconazole Etravirine, when used concomitantly with Ketoconazole (and other azole derivatives), may experience an increase in serum concentration. Ketoconazole (and other azole derivatives), when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to monitor etravirine therapy for toxicity.
Lapatinib Lapatinib, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid this combination.
Lidocaine Lidocaine, when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to monitor lidocaine therapy.
Linagliptin Linagliptin, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy if possible, and to monitor linagliptin therapy if concurrent use cannot be avoided.
Lopinavir Etravirine, when used concomitantly with protease inhibitors, may experience a decrease in serum concentration. Protease inhibitors, when used concomitantly with etravirine, may experience an increase in serum concentration. Ritonavir boosting of etravirine therapy is a requirement to concurrent therapy. In addition, it is recommended to monitor serum concentrations of the antiretrovirals, as well as to monitor antiretroviral therapy for efficacy.
Lovastatin Lovastatin, when administered concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to monitor continued efficacy of lovastatin therapy.
Lurasidone Concomitant therapy with a CYP3A4 inducer will decrease levels of lurasidone. Coadministration with lurasidone is contraindicated.
Lurasidone Lurasidone, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Maraviroc Maraviroc, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Methadone Methadone, when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to monitor methadone therapy for decrease effectiveness and symptoms of withdrawal.
Mexiletine Mexiletine, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to monitor mexiletine therapy for reduced effectiveness.
Mifepristone Mifepristone, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Nevirapine Nevirapine may cause a significant decrease in plasma levels of etravirine and a loss of efficacy. Combination of two NNRTIs has not been demonstrated to be of benefit to HIV therapy.
Nifedipine Nifedipine, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to monitor nifedipine therapy for reduced effectiveness.
Nilotinib Nilotinib, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Nisoldipine Nisoldipine, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Paclitaxel Paclitaxel, when used concomitantly with NNRTIs, may experience an increase in serum concentration. It is recommended to monitor for paclitaxel toxicity.
Pazopanib Pazopanib, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Peginterferon alfa-2a Etravirine (a CYP2C9 substrate), when used concomitantly with peginterferon alfa-2a, may experience a decrease in serum concentration. It is recommended to monitor effectiveness of etravirine therapy.
Perampanel Perampanel, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Phenobarbital Etravirine, when used concomitantly with phenobarbital, may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Phenytoin Etravirine, when used concomitantly with phenytoin, may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Praziquantel Praziquantel, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Praziquantel Praziquantel, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Primidone Etravirine, when used concomitantly with Primidone (primarily metabolized to phenobarbital), may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Propafenone Propafenone, when used concomitantly with Etravirine, may experience a decrease in serum concentration. It is recommended to monitor for continued efficacy of propafenone therapy.
Quetiapine Quetiapine, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to increase quetiapine dosage if concurrent therapy is required.
Quinidine Quinidine, when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to monitor quinidine therapy.
Rifabutin Etravirine may experience a decrease in serum concentration. It is recommended to monitor etravirine therapy for efficacy. The combination of rifabutin and etravirine therapy is contraindicated if a protease inhibitor which is ritonavir boosted is also being used.
Rifamycin Cgp 4832 Etravirine, when used concomitantly with rifamycin, may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Rilpivirine Rilpivirine, when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy. Use of rilpivirine and other NNRTIs is containdicated.
Rivaroxaban Rivaroxaban may experience a decrease in serum concentration. U.S prescribing information recommends avoiding concurrent therapy.
Roflumilast Affects CYP3A4 metabolism, decreases level or effect of roflumilast.
Roflumilast Roflumilast, when used concomitantly with etravirine, may experience a decrease in serum concentration. U.S prescribing information recommends avoiding concurrent therapy.
Romidepsin Romidepsin, when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Saquinavir Etravirine, when used concomitantly with protease inhibitors, may experience a decrease in serum concentration. Protease inhibitors, when used concomitantly with etravirine, may experience an increase in serum concentration. Ritonavir boosting of etravirine therapy is a requirement to concurrent therapy. In addition, it is recommended to monitor serum concentrations of the antiretrovirals, as well as to monitor antiretroviral therapy for efficacy.
Sildenafil Sildenafil (and other phosphodiesterase 5 inhibitors), when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to monitor the efficacy of sildenafil therapy.
Simvastatin Simvastatin, when administered concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to monitor continued efficacy of simvastatin therapy.
Sorafenib Sorafebib, when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
St. John's Wort Etravirine may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Tamsulosin Etravirine, a CYP3A4 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Etravirine is initiated, discontinued, or dose changed.
Telaprevir Telaprevir, when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to monitor telaprevir therapy closely.
Ticagrelor Etravirine, when used concomitantly with ritonavir boosted ticagrelor, may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Tipranavir Tipranavir, co-administered with Ritonavir, may decrease the effect of Etravirene by decreasing Etravirene serum concentration. Concomitant therapy should be avoided.
Tolterodine Etravirene may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity.
Tolvaptan Tolvaptan may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Toremifene Toremifene, when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Tramadol Tramadol,when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration and efficacy due to increased tramadol metabolism and clearance.
Trazodone The CYP3A4 inducer, Etravirene, may decrease Trazodone efficacy/toxicity by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Etravirine is initiated, discontinued or dose changed.
Vandetanib Decreases levels of vandetanib by affecting CYP3A4 metabolism. Contraindicated.
Vincristine Vincristine, when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Voriconazole Etravirine, when used concomitantly with variconazole, may experience an increase in serum concentration due to decreased metabolism of etravirine. Voriconazole, when used concomitantly with etravirine (a CYP2C19 inhibitor), may experience a decrease in serum concentration. Monitor for changes in efficacy and toxicity of both agents if concomitant therapy is initiated, modified or discontinued.
Zuclopenthixol Zuclopenthixol (especially oral dosage form) may experience a decrease in serum concentration when used concomitantly with etravirine. It is recommended to monitor zuclopenthixol therapy for efficacy.

Liều Lượng & Cách Dùng : Tablet - Oral - 100mg
Tablet - Oral - 200mg
Tablet - Oral - 25mg

Dữ Kiện Thương Mại

Nhà Sản Xuất

Công ty : Janssen

Sản phẩm biệt dược : Intelence

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB06414

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D04112

National Drug Code Directory

http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/53808-0787-1

Wikipedia

http://en.wikipedia.org/wiki/Etravirine

RxList

http://www.rxlist.com/intelence-drug.htm

Drugs.com

http://www.drugs.com/cdi/etravirine.html

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