Sustiva

This page contains recent news articles, when available, and an overview of Sustiva but does not offer medical advice. You should contact your physician with regard to any health issues or concerns.

Overview:

Sustiva (when available)

Pharmacology and use:
Efavirenz (dideoxyinosine, ddI) is an oral nucleoside reverse transcriptase inhibitor (NRTI). It is a synthetic purine derivative and, similar to zidovudine, zalcitabine, and stavudine. Efavirenz was originally approved specifically for the treatment of HIV infections in patients who failed therapy with zidovudine. Currently, the CDC recommends that Efavirenz be given as part of a three-drug regimen that includes another nucleoside reverse transcriptase inhibitor (e.g., lamivudine, stavudine, zidovudine) and a protease inhibitor or efavirenz when treating HIV infection. For use in combination treatment of HIV infection (AIDS)

Mechanism Of Action:
Similar to zidovudine, Efavirenz inhibits the activity of viral RNA-directed DNA polymerase (i.e., reverse transcriptase). Antiviral activity of Efavirenz is dependent on intracellular conversion to the active triphosphorylated form. The rate of Efavirenz phosphorylation varies, depending on cell type. It is believed that inhibition of reverse transcriptase interferes with the generation of DNA copies of viral RNA, which, in turn, are necessary for synthesis of new virions. Intracellular enzymes subsequently eliminate the HIV particle that previously had been uncoated, and left unprotected, during entry into the host cell. Thus, reverse transcriptase inhibitors are virustatic and do not eliminate HIV from the body. Even though human DNA polymerase is less susceptible to the pharmacologic effects of triphosphorylated Efavirenz, this action may nevertheless account for some of the drug's toxicity.

News Articles on Efavirenz

Bristol-Myers spent $809K lobbying gov't in 2Q  -  ‎Aug 24, 2009‎
Bristol-Myers sells Atripla and Sustiva for HIV infection. Bristol-Myers also lobbied against the government negotiating discounts for drugs sold to seniors Forbes

Cipla receives USFDA nod for Efavirenz  -  ‎Aug 5, 2009‎
Efavirenz (brand names Sustiva and Stocrin) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and is used as part of highly active antiretroviral Myiris.com

Detectable HIV Levels Don't Necessarily Increase the Risk of ...  -  ‎Aug 25, 2009‎
Roughly half of those on treatment were taking a regimen that included efavirenz (found in Sustiva and Atripla), which can affect cognitive function in some AIDSmeds.com HIV/AIDS Treatment News

5 Stocks Making Cash  -  ‎Aug 12, 2009‎
A combination of Gilead's Truvada and Bristol-Myers Squibb's (NYSE: BMY) Sustiva, the antiretroviral Atripla is the most prescribed treatment for HIV, Motley Fool

When progress comes at a price…  -  ‎Aug 13, 2009‎
In both cases the writers compared the results of a “conventional�? first line treatment – of which the third component was either Efavirenz (Sustiva®) or Destination Santé

More evidence of bone loss with HIV therapy, more confusion over ...  -  ‎Aug 13, 2009‎
Participants were randomised to receive either efavirenz (Sustiva, also marketed as Stocrin) or Kaletra along with AZT plus 3TC (lamivudine, Epivir). Aidsmap

Matrix Labs gets tentative USDFA nod for HIV drugs  -  ‎Aug 14, 2009‎
Efavirenz (brand names Sustiva and Stocrin) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and is prescribed for the treatment of a human TopNews

Sida : l'antirétroviral raltegravir sera t-il en première ligne ?  -  ‎Aug 12, 2009‎
...d'un traitement de première ligne « conventionnel » - dont le troisième composant était soit l'efavirenz (Sustiva®) soit le raltegravir (Isentress®). Futura Sciences

Merck & Co: dosing regime may hinder Isentress uptake  -  14 Jul 2009
STARTMRK study in which the safety and efficacy of Isentress was compared to leading first-line agent Sustiva (efavirenz) in this patient population. Trading Markets (press release)

中科�?�臣：�?欣集团强势入主资本整�?�大幕开�?�  -  14 Jul 2009
...公�?�主�?产�?02A是一�?环丙基乙炔化�?�物，该产�?是生产特效抗艾滋病�?�物Sustiva的�?�?中间体，因而具备抗艾滋病概念。目�?，艾滋病在亚洲和中国�?步�?行并呈现快速上�?� 凤凰网

Merck HIV drug Isentress gets full US approval  -  ‎Jul 9, 2009‎
The approval was based on a 48-week study comparing patients who took Isentress with patients who took another HIV drug, Sustiva. Both groups also took two Forbes

Isentress Gets FDA Approval for Treatment Newbies  -  ‎Jul 10, 2009‎
The approval was based on 48 week data from the STARTMRK study comparing Isentress and Truvada (tenofovir plus emtricitabine) with Sustiva (efavirenz) and AIDSmeds.com HIV/AIDS Treatment News

Stepped Dosing Lessens Neuropsychiatric Effects of Efavirenz  -  ‎Jul 6, 2009‎
NJ, July 6 -- A stepwise dosing schedule eases the neuropsychiatric side effects of the HIV drug efavirenz (Sustiva), a randomized trial showed. MedPage Today

MediaVest Wins $400 Million Bristol-Myers Squibb Account  -  ‎Jun 30, 2009‎
Some of the pharma giant's biggest selling brands include Plavix, Abilify, Reyataz and Sustiva. This marks the second time in as many months that MediaVest AdAge.com (subscription)

Anti-HIV and anti-cancer drugs derived from Borneo rainforest ...  -  ‎Jun 28, 2009‎
Approved NNRTIs include Viramune® (nevirapine) from Boehringer Ingelheim, Sustiva® (efavirenz) from Bristol-Myers Squibb, and Rescriptor® (delavirdine) from Mongabay.com

BMY -10 Companies With Ironclad Balance Sheets  -  ‎Jun 28, 2009‎
The Pharmaceuticals segment offers cardiovascular products, including PLAVIX, AVAPRO/AVALIDE, and PRAVACHOL; virology products comprising REYATAZ, SUSTIVA, TransWorldNews (press release)

VAOIG: VA PHARMACY INVENTORY CONTROL NON-EXISTENT  -  ‎Jun 23, 2009‎
Four of these drugs—Sustiva, Zyprexa, Ultram, and Levitra—are considered at increased risk for diversion. We also included the anti-clotting drug Plavix in VA Watchdog dot Org

Viagra rivals add hours of hope for men - $1.15 per PILL  -  ‎Jun 30, 2009‎
...darunavir (Prezista), efavirenz (Sustiva), nevirapine (Viramune), indinavir (Crixivan), saquinavir (Invirase, Fortovase), lopinavir/ritonavir (Kaletra), Toute la Poésie

FUNDVIEW-Franklin fund sees opportunity in cheap biotechs  -  ‎Jul 6, 2009‎
Sales of the newer Atripla, which combines Truvada with Bristol-Myers Squibb Co's Sustiva into a single pill, jumped 57 percent in the same period. Forbes

Ciencia y tecnología del 3 de julio  -  ‎Jul 2, 2009‎
El medicamento, bautizado Atripla, combina los antirretrovirales efavirenz (comercializado con el nombre de Sustiva), emtricitabina (Emtriva) y tenofovir Costa Rica Hoy

疫苗生产上市公�?�相关分�?  -  ‎Jun 18, 2009‎
...中科�?�臣(资讯行情论�?�)(600490)：公�?�主�?产�?02A是一�?环丙基乙炔化�?�物，该产�?是生产特效抗艾滋病�?�物Sustiva的�?�?中间体。245化学�??称为�?�氟苯甲酸，是生产一类阿里巴巴

Gilead Initiates Phase II Clinical Trial Of Integrase-Based ...  -  20 Apr 2009
Atripla contains the components Truvada (emtricitabine and tenofovir disoproxil fumarate) and Sustiva (efavirenz), co-formulated as a single tablet. Medical News Today (press release)

Gilead initiiert Phase II klinischer Studie zur HIV-Behandlung ...  -  20 Apr 2009
Atripla enthält die Komponenten Truvada (Emtricitabin und Tenofovir-Disoproxil-Fumarat) und Sustiva (Efavirenz) in einer Formulierung als Einzeltablette. Business Wire (press release)

DEALWATCH: Dull Pharma JV May Become Alluring Spin-Off, Sale  -  ‎Apr 16, 2009‎
...(BMY) has two big HIV drugs, Reyataz and Sustiva, which together generated 2008 sales equal to the JV. And importantly, Gilead and Bristol's HIV products Wall Street Journal

Drug to Battle AIDs Abused for Pleasure  -  ‎Apr 7, 2009‎
Efavirenz is a prescription drug with the brand names of Sustiva and Stocrins. It is used as part of an antiviral cocktail for patients with HIV and AIDS. Health Jackal

A Boon For HIV Drugs?  -  ‎Apr 9, 2009‎
Earlier use of antiviral drugs like Viread, Sustiva and Combivir would boost sales for their makers. The biggest winner would likely be Foster City, Calif. Forbes

Bone loss during HIV treatment most associated with protease ...  -  ‎Apr 17, 2009‎
The prescribed NNRTIs were either efavirenz (Sustiva) or nevirapine (Viramune). With the exception of d4T and ddC, all the licensed NRTIs were available for Aidsmap

Gilead Initiates Phase II Clinical Trial of Integrase-Based ...  -  ‎Apr 17, 2009‎
The most significant adverse events observed in patients treated with Sustiva are nervous system symptoms, psychiatric symptoms and rash. PR-Inside.com (Pressemitteilung)

Gilead initie un essai clinique de Phase II avec un régime ...  -  ‎Apr 19, 2009‎
L'Atripla contient les composants Truvada (emtricitabine et fumarate de ténofovir disoproxil) et Sustiva (éfavirenz), en formule commune dans un comprimé Euroinvestor

Bristol Names New President, COO  -  ‎Mar 3, 2009‎
...fourth-quarter earnings in January, attributable to the sale of its ImClone stake and to sales of key drugs, including Plavix, HIV drug Sustiva and Abilify. TheStreet.com

Ardea Biosciences Reports Progress of Clinical Development ...  -  ‎Mar 13, 2009‎
...which can lead to increased side effects in African-Americans, have been documented with efavirenz (Sustiva(R), Bristol-Myers Squibb). StreetInsider.com (subscription)

Pharmacist to help fraud prosecution  -  ‎Mar 4, 2009‎
Drugs obtained illegally by Shoemaker and his associates include Sustiva, Norvir, Neupogen, Viramune and Truvada, according to court documents. Gwinnett Daily Post

Endothelial dysfunction in Italian cohort caused by HIV, not ...  -  ‎Mar 8, 2009‎
Eighty-six per cent of the NNRTI group took efavirenz (Sustiva), and 14% nevirapine (Viramune). The researchers found further evidence of the impact of HIV Aidsmap

GSK归�?��?��?�抗艾严冬市场王者地�?�?�?  -  ‎Mar 16, 2009‎
...尽管�?�核苷类逆转录酶抑制剂被认为是HIV感染治疗常用的一线治疗方案，但该类�?�物中第一个被批准上市的�?�物�?�?�韦仑（efavirenz，Sustiva）�?�已�?出现了�?�?�的倾�?�，中国医药网

La visibilità degli utili fra le biotecnologie rimane notevole  -  ‎Feb 24, 2009‎
L’incremento è stato indotto dalla vendita dei farmaci per il trattamento dell’HIV Truvada e Atripla, una somministrazione unica di Truvada e Sustiva fondionline.it

Bristol-Myers Posts Q4 Profit Reversing Year-ago Loss - Update  -  Jan 27, 2009
The virology portfolio, led by Sustiva and Baraclude also demonstrated consistent growth worldwide, the company said. Global net sales of Plavix for the RTT News,

Gilead Sciences Inc. Q4 2008 Earnings Call Transcript  -  Jan 27, 2009
As Sustiva's one of the preferred third-agents, the combined product of Truvada plus Sustiva, namely Atripla, provides a patient's complete regimen in one Seeking Alpha,

Pharma Earnings In Q4 - Healthy Or Ailing?  -  Jan 25, 2009
Bristol Myers' key products include blood thinner drug Plavix, anti-hypertension drugs Avapro/Avalide, HIV drugs Reyataz and Sustiva, antipsychotic drug Trading Markets (press release),

One-a-day regimens mean better adherence for patients starting HIV ...  -  Jan 29, 2009
...versus twice-daily abacavir/3TC/AZT (Trizivir); and between d4T (stavudine, Zerit)/3TC (lamivudine, Epivir)/efavirenz (Sustiva), and any other regimen. Aidsmap,

US Latinos have more unfavourable metabolic and body fat changes ...  -  Jan 16, 2009
They also controlled for cumulative time on ten antiretroviral drugs: indinavir (Crixivan), nelfinavir (Viracept), ritonavir (Norvir), efavirenz (Sustiva), Aidsmap,

Gilead aiming to put four HIV drugs in one pill  -  Jan 14, 2009
...by another of its combination pills Atripla (co-marketed with Bristol-Myers Squibb) which contains tenofovir, emtricitabine and efavirenz (Sustiva). Aidsmap,

�?牌�?�陆续专利失效医�?�巨头“金弹�?攻势�?�?  -  Feb 3, 2009
...而在这几个领域里，百时美施贵�?�?�有相应的�?�物出售，其中包括全�?�第二大畅销�?�物波立维（Plavix）和Coumadin，抗艾滋病�?�物Atripla和Sustiva �?��?,

Chat avec Christine Katlama sur Yagg: Le dialogue avec les ...  -  Jan 23, 2009
Mais des amis me disent que le Sustiva rentre dans la composition du comprimé, et peut créer des perturbations d'humeur… Je prends déjà du lithium, yagg.typepad.com,

Gleevec wins new FDA indication; Drug shortage could boost Roche's ...  -  Dec 22, 2008
Report > Aurobindo Pharma won tentative FDA approval to manufacture and market the HIV drug efavirenz, the generic form of branded drugs Sustiva and Stocrin FiercePharma,

The New America  -  Dec 16, 2008
Gilead sells the drug with partner Bristol Myers-Squibb (BMY), which developed Sustiva. Like most drug companies, Gilead's sales come mostly from the US, Investor's Business Daily (subscription)

Gilead sues Teva over HIV drug patent  -  Dec 15, 2008
...s Sustiva. Truvada sales reached $549.1 million during the third quarter, making up 40 percent of the company's revenue during that period. BusinessWeek

Clinic Roundup  -  Dec 15, 2008
The studies will compare TMC278, given as a once-daily oral tablet, to Sustiva (efavirenz, Bristol-Myers Squibb Co.), when administered with a background TMCnet

Citi Upgrades Bristol-Myers Squibb (BMY) to Buy  -  Dec 10, 2008
Currently marketed drugs in this category would include Abilify for schizophrenia, Reyataz and Sustiva for HIV, Orencia for rheumatoid arthritis, StreetInsider.com (subscription),

12月23日�?券通异动股解密评级�?�考  -  Dec 22, 2008
...从基本�?�看，公�?�主�?产�?02A是一�?环丙基乙炔化�?�物，该产�?是生产特效抗艾滋病�?�物Sustiva 新浪网,

Gilead就HIV�?��?专利起诉Teva  -  Dec 15, 2008
Emtriva与Viread也是三�?�一的HIV治疗�?�Atripla，以�?�百时美施贵�?生产的Sustiva 新浪网,

2008-12-11 0:31:58 �?��?:�?�年人(Qnr.Cn) 作者:Qnr.Cn  -  Dec 10, 2008
They have ____4____ a single pill that combines three drugs currently on the market.3 Bristol-Myers Squibb sells one of them ____5____ the name of Sustiva �?�年人,

Gilead就HIV藥�?專利起訴Teva  -  Dec 15, 2008
Emtriva與Viread也是三�?�一的HIV治療藥Atripla，以�?�百時美施貴寶生產的Sustiva 新浪網,

Advierte Ercilia León: Mujeres embarazadas deben hacerse ...  -  Dec 18, 2008
No obstante, algunos de estos fármacos, incluyendo el efavirenz (Sustiva) y la hidroxiurea, suelen estar contraindicados durante el embarazo debido a un Diario el Tiempo (Venezuela),

Celsentri en première intention  -  Dec 16, 2008
La «non-infériorité virologique» de l'anti-VIH maraviroc (Celsentri, des laboratoires Pfizer) comparé à l'éfavirenz (Sustiva, des laboratoires BMS) est TÊTU,

Brand Names/Synonyms:
Sustiva is also known by the following brand names and/or synonymsDMP 266; DMP-266; EFV; Efavirenz; Stocrin; Sustiva

Drug Category:
Sustiva is categorized under the following by the FDA: Anti-HIV Agents; Nonnucleoside Reverse Transcriptase Inhibitors; ATC:J05AG03

Dosage Forms:
TABLET, CAPSULE

Absorption:
Not Available

Interactions:
-->Interactions for Efavirenz:

Efavirenz has been shown in vivo to induce CYP3A4. Other compounds that are substrates of CYP3A4 may have decreased plasma concentrations when coadministered with SUSTIVA (efavirenz). In vitro studies have demonstrated that efavirenz inhibits 2C9, 2C19, and 3A4 isozymes in the range of observed efavirenz plasma concentrations. Coadministration of efavirenz with drugs primarily metabolized by these isozymes may result in altered plasma concentrations of the coadministered drug. Therefore, appropriate dose adjustments may be necessary for these drugs.

Drugs which induce CYP3A4 activity (eg, phenobarbital, rifampin, rifabutin) would be expected to increase the clearance of efavirenz resulting in lowered plasma concentrations. Drug interactions with SUSTIVA are summarized in Table 5.

Table 5^a: Drugs That Should Not Be Coadministered With SUSTIVA
Drug Class		Drugs Within Class Not To Be Coadministered With SUSTIVA
Antihistamines Benzodiazepines GI Motility Agents Anti-Migraine Antifungal		astemizole midazolam, triazolam cisapride ergot derivatives voriconazole
Established Drug Interactions
Drug Name	Effect	Clinical Comment
Atazanavir	¯atazanavir	When coadministered with SUSTIVA in treatment-naive patients, the recommended dose of atazanavir is 300 mg with ritonavir 100 mg and SUSTIVA 600 mg (all once daily). Dosing recommendations for SUSTIVA and atazanavir in treatment-experienced patients have not been established.
Established Drug Interactions (continued)
Drug Name	Effect	Clinical Comment
Clarithromycin	¯clarithromycin concentration	Plasma concentrations decreased by SUSTIVA; clinical significance unknown. In uninfected volunteers, 46% developed rash while receiving SUSTIVA and clarithromycin. No dose adjustment of SUSTIVA is recommended when given with clarithromycin. Alternatives to clarithromycin, such as azithromycin, should be considered. Other macrolide antibiotics, such as erythromycin, have not been studied in combination with SUSTIVA.

	14-OH metabolite concentration
Indinavir	¯indinavir concentration	The optimal dose of indinavir, when given in combination with SUSTIVA, is not known. Increasing the indinavir dose to 1000 mg every 8 hours does not compensate for the increased indinavir metabolism due to SUSTIVA. When indinavir at an increased dose (1000 mg every 8 hours) was given with SUSTIVA (600 mg once daily), the indinavir AUC and C_min were decreased on average by 33-46% and 39-57%, respectively, compared to when indinavir (800 mg every 8 hours) was given alone.
Lopinavir/ritonavir	¯lopinavir concentration	A dose increase of lopinavir/ritonavir to 533/133 mg (4 capsules or 6.5 mL) twice daily taken with food is recommended when used in combination with SUSTIVA.
Methadone	¯methadone concentration	Coadministration in HIV-infected individuals with a history of injection drug use resulted in decreased plasma levels of methadone and signs of opiate withdrawal. Methadone dose was increased by a mean of 22% to alleviate withdrawal symptoms. Patients should be monitored for signs of withdrawal and their methadone dose increased as required to alleviate withdrawal symptoms.
Ethinyl estradiol	ethinyl estradiol concentration	Plasma concentrations increased by SUSTIVA (efavirenz); clinical significance unknown. Because the potential interaction of efavirenz with oral contraceptives has not been fully characterized, a reliable method of barrier contraception should be used in addition to oral contraceptives.
Rifabutin	¯rifabutin concentration	Increase daily dose of rifabutin by 50%. Consider doubling the rifabutin dose in regimens where rifabutin is given 2 or 3 times a week.
Rifampin	¯efavirenz concentration	Clinical significance of reduced efavirenz concentrations unknown.
Ritonavir	ritonavir concentration	Combination was associated with a higher frequency of adverse clinical experiences (eg, dizziness, nausea, paresthesia) and laboratory abnormalities (elevated liver enzymes). Monitoring of liver enzymes is recommended when SUSTIVA is used in combination with ritonavir.

	efavirenz concentration

Saquinavir	¯saquinavir concentration	Should not be used as sole protease inhibitor in combination with SUSTIVA.
Sertraline	¯sertraline concentration	Increases in sertraline dose should be guided by clinical response.
Other Potentially Clinically Significant Drug or Herbal Product Interactions With SUSTIVA^b
Anticoagulants: Warfarin		Plasma concentrations and effects potentially increased or decreased by SUSTIVA.
Anticonvulsants: Phenytoin Phenobarbital Carbamazepine		Potential for reduction in anticonvulsant and/or efavirenz plasma levels; periodic monitoring of anticonvulsant plasma levels should be conducted.
Antifungals: Itraconazole Ketoconazole		Drug interaction studies with SUSTIVA and these imidazole and triazole antifungals have not been conducted. SUSTIVA has the potential to decrease plasma concentrations of itraconazole and ketoconazole.
Anti-HIV protease inhibitors: Saquinavir/ritonavir combination		No pharmacokinetic data are available.
Amprenavir		SUSTIVAhas the potential to decrease serum concentrations of amprenavir.
Non-nucleoside reverse transcriptase inhibitors		No studies have been performed with other NNRTIs.
St. Johnís wort (Hypericum perforatum)		Expected to substantially decrease plasma levels of efavirenz;has not been studied in combination with SUSTIVA.
^a See Tables 1 and 2.
^b This table is not all-inclusive.

Other Drugs: Based on the results of drug interaction studies, no dosage adjustment is recommended when SUSTIVA (efavirenz) is given with the following: aluminum/magnesium hydroxide antacids, azithromycin, cetirizine, famotidine, fluconazole, lamivudine, lorazepam, nelfinavir, paroxetine, and zidovudine.

Specific drug interaction studies have not been performed with SUSTIVA and NRTIs other than lamivudine and zidovudine. Clinically significant interactions would not be expected since the NRTIs are metabolized via a different route than efavirenz and would be unlikely to compete for the same metabolic enzymes and elimination pathways.

Chemical IUPAC Name:
8-chloro-5-(2-cyclopropylethynyl)-5-(trifluoromethyl)-4-oxa-2-azabicyclo[4.4.0]deca-7,9,11-trien-3-one

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