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SustivaThis 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) 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 IAC: Efavirenz (Sustiva) the Pick in Severely Immunocompromised ... - Aug 5, 2008 5 -- In HIV patients who begin treatment with a damaged immune system, a drug regimen based on efavirenz (Sustiva) remains the best choice, a researcher MedPage Today, IAC: Raltegravir (Isentress) Matches Standard Initial Care at 96 Weeks - Aug 6, 2008 After 96 weeks of treatment, raltegravir had a virological effect that was almost identical to standard therapy with efavirenz (Sustiva), according to Marty MedPage Today, Gilead to sell HIV drug in 12 additional countries - Aug 1, 2008 ...s Sustiva. Merck & Co. distributes the drug in 94 developing countries and Bristol-Myers sells it in Europe, but under the new agreement, Gilead will take CNNMoney.com Ardea Biosciences Presents Phase 2a Antiviral Activity Data for ... - Aug 7, 2008 ..."We look forward to further evaluating RDEA806 and are on track to begin a Phase 2b study comparing once daily doses of RDEA806 to efavirenz (SUSTIVA(R), MarketWatch IAC: TB Drug Alters Power of HIV Medication - Aug 3, 2008 Note that this study found that taking rifampin can reduce the efficacy of nevirapine (Viramune) but not efavirenz (Sustiva). On the other hand, MedPage Today, BMS : save the children’s lives, not your profits - Aug 4, 2008 BMS stopped the distribution of the 100 mg paediatric formulation of efavirenz, known in some countries as Sustiva. Though, this drug is the most suited for Act Up-Paris, HIV Drug Resistance More Common than Testing Suggests - Jul 29, 2008 ...and colleagues studied drug-naive patients who had taken part in two trials of the non-nucleoside reverse transcriptase inhibitor efavirenz (Sustiva). MedPage Today, Cost-cutting helps B-MS profits and more cuts are planned - Jul 25, 2008 Sales of its Sustiva (efavirenz) franchise rose 21% to $282 million and Reyataz (atazanavir) was up 28% to $324 million. The cancer agent Erbitux Pharma Times (subscription), Abbott Study Shows Investigational Heat-Stable Norvir(R) Tablet ... - Aug 7, 2008 KALETRA should not be given once-daily in combination with Sustiva(R) (efavirenz), Viramune(R) (nevirapine), Agenerase(R) (amprenavir), fosamprenavir, FOXBusiness Bill Clinton Says Health System Fails High-Risk AIDS Patients - Aug 4, 2008 For the drug efavirenz, sold by Bristol Myers-Squibb Co. as Sustiva, the chemists found an alternative chemical pathway in the synthesis process to replace Bloomberg IAC: Researchers, Company Clash Over HIV Drug Combination - Aug 8, 2008 Dr. Sax said the study initially had four arms, comparing the two fixed-dose pills with placebo in combination with either efavirenz (Sustiva) or atazanavir MedPage Today, IAC: Unboosted Atazanavir HIV Regimen Found Inferior - Aug 8, 2008 It proved inferior to a combination of zidovudine (Retrovir) and 3TC (Epivir), both twice daily, combined with daily efavirenz (Sustiva) in its ability to MedPage Today, Two new NNRTIs look promising in early clinical trials - Aug 8, 2008 ...against a variety of HIV strains with mutations conferring resistant to other NNRTIs, including the commonly prescribed efavirenz (Stocrin or Sustiva). Aidsmap, Ardea reports encouraging results from Phase IIa HIV study - Aug 8, 2008 ...to efavirenz (Sustiva, Stocrin) in first-line patients receiving background treatment with Truvada (emtricitabine and tenofovir disoproxil fumarate), Trading Markets (press release), Abbott's Kaletra(R) Tablet Dosed Once-Daily or Twice-Daily ... - Aug 5, 2008 KALETRA should not be given once-daily in combination with Sustiva(R) (efavirenz), Viramune(R) (nevirapine), Agenerase(R) (amprenavir), fosamprenavir, FOXBusiness How does abacavir/3TC compare to tenofovir/FTC? ACTG5202 and GSK ... - Aug 7, 2008 In the ongoing US AIDS Clinical Trials Group (ACTG) Study A5202, each of these two nucleoside pairs has been paired with either efavirenz (Sustiva) or Aidsmap, IAC: HIV Care Guidelines Expand Treatment Eligibility - Aug 3, 2008 The preferred NNRTI is efavirenz (Sustiva), but several PIs are suggested, including lopinavir (Kaletra), atazanavir (Reyataz), fosamprenavir (Lexiva), MedPage Today, New HIV/AIDS Guidelines Suggest Earlier Treatment - Aug 3, 2008 The authors of the guidelines also recommended that frontline regimens be individualized, and that certain drugs such as Sustiva (efavirenz) be given high U.S. News & World Report, Efficacy and Tolerability Profile Consistent With Data Seen in ... - Aug 7, 2008 ...in 83 percent of previously untreated (treatment-naïve) HIV-infected patients which was comparable to that seen with efavirenz (Sustiva®/STOCRIN®)*, WebWire (press release), Merck Responds to Aids Activists' Pleas; Reduces Price of Stocrin ... - Aug 2, 2008 Merck cut its price of Stocrin (efavirenz, branded as Sustiva in the US) in Mexico by 40% from 777 pesos per patient monthly to 468 pesos (roughly from MarketWatch InvestSource, Inc.: CEO, Dennis Tan of Uranium 308 Corp. Featured ... - Aug 6, 2008 ...of previously untreated (treatment-nave) HIV-infected patients which was comparable to that seen with efavirenz (Sustiva /STOCRIN )*, which reduced HIV Trading Markets (press release), Lipodystrophy common, but does not affect adherence in Thai patients - Aug 4, 2008 The rest (1.1%) were started on d4t, lamivudine and efavirenz (Sustiva). After three years 73.7% were still on d4t, lamivudine and nevirapine and 6.4% were Aidsmap, Lilly, Bristol-Myers Profit on Psychiatric Drugs (Update1) - Jul 24, 2008 Revenue from the AIDS medicine Reyataz climbed 28 percent to $324 million and the AIDS therapy Sustiva climbed 21 percent to $282 million. Bloomberg Gilead Sciences 2nd-qtr profit rises 8.6 pct - Jul 17, 2008 Sales of the newer Atripla, which combines Truvada with Bristol-Myers Squibb Co's Sustiva into a single pill, rose 67 percent to $355.1 million. guardian.co.uk, Earnings Preview: Gilead Sciences - Jul 16, 2008 ...(nyse: BMY - news - people )'s Sustiva. The company's drugs dominate the HIV treatment market, with some Wall Street estimates placing more than half of all Forbes, Fitch Expects Bristol-Myers Squibb's Ratings to be Unaffected by ... - Jul 31, 2008 Revenue growth will be led by Bristol-Myers Squibb's five top-selling products: Plavix, Avapro/Avalide, Abilify, Reyataz and Sustiva, offset by loss of PR-Inside.com (Pressemitteilung), Bristol-Myers Squibb Co. Q2 2008 Earnings Call Transcript - Jul 27, 2008 SUSTIVA Franchise, sales were up by 21% globally behind the strong performance of ATRIPLA. Please take note that the US sales for HIV are somewhat flat Seeking Alpha, Gilead Sciences, Inc. Q2 2008 Earnings Call Transcript - Jul 31, 2008 Combivir continued regiments comprised 35% of switch and Kivexa plus Sustiva comprised 19% of switch patients. Truvada has continued to build on the solid Seeking Alpha, Analyst Actions: Google, Overstock.Com, Gilead Sciences - Jul 21, 2008 Given the maturity of GILD's core HIV franchise, Yang expects HIV drug sales growth [excluding Sustiva] in out years to be much tamer [estimated average istockAnalyst.com, Genital shedding of HIV in women with undetectable viral load ... - Jul 17, 2008 HIV treatment consisted of AZT (zidovudine, Retrovir) or d4T (stavudine, Zerit) with 3TC (lamivudine, Epivir) and efavirenz (Sustiva). Aidsmap, WHITEHOUSE STATION, NJ--(BUSINESS WIRE)-- - Aug 5, 2008 Canada, United Kingdom, Republic of Ireland, France (continental only), Spain, Italy and Germany, and markets efavirenz under its trademark Sustiva(R). StreetInsider.com (subscription), Des enfants privés d'un traitement VIH adapté - Aug 6, 2008 Profitant de la Conférence mondiale de Mexico, un collectif d'associations (1) dénonce l'arrêt de la commercialisation du médicament Sustiva sous forme de L'Express, Act Up-Paris et Health GAP (Global Access Project) offrent des ... - Aug 7, 2008 BMS a stoppé la distribution de la formulation pédiatrique de 100 mg de l’éfavirenz, connu dans certains pays sous le nom de Sustiva, malgré le fait que ce Act Up-Paris, Et toujours - Jul 31, 2008 BKVIR est une étude pilote non comparative, évaluant l’efficacité d’une trithérapie antirétrovirale en une prise journalière associant Truvada® et Sustiva® Act Up-Paris, BMS sacrifie la vie des enfants à ses profits - Aug 3, 2008 BMS a arrêté la commercialisation d’une formulation pédiatrique, à 100 mg, de l’efavirenz, connu dans certains pays sous le nom de Sustiva. Act Up-Paris, Espoirs en résistance majeure - Jul 31, 2008 Analogues non nucléosidiques inhibiteurs de la transcriptase inverse : Rescriptor® (delavirdine), Sustiva® (efavirenz), Viramune® (nevirapine). Act Up-Paris, Ð?мериканÑ?кие фармацевты не Ñ?ошлиÑ?ÑŒ в цене - Aug 4, 2008 Ð’ портфолио компании входÑ?Ñ‚ такие препараты, как Avapro, Enfamil, Plavix, Sustiva и другие. Отметим, Bristol-Myers Squibb длительное времÑ? Ñ?влÑ?лаÑ?ÑŒ Комп&ньон.online (преÑ?Ñ?-релиз), Merck responde a las demandas de activistas del Sida; reduce el ... - Aug 4, 2008 Merck redujo el precio de su Stocrin (efavirenz, bajo la marca Sustiva en los Estados Unidos) en México en un 40%, de 777 pesos por mes por paciente a 468 Business Wire (press release), > Actualités > Ouverture à Mexico de la 17e Conférence ... - Aug 4, 2008 ...contre sa décision d’arrêter la commercialisation d’une version pédiatrique de l’Efavirenz, un antirétroviral également connu sous le nom de Sustiva. EspaceInfirmier.com, Conferenza Internazionale sull'AIDS. Dalla conferenza: Alessandra ... - Aug 4, 2008 Dopo la minaccia annunciata, la Merck Sharp & Dome ha annunciato che ridurrà del 41% il Sustiva e del 37% quello del nuovo inibitore delle integrasi ConfiniOnline, RECHERCHE RAPIDE PAR ORGANISME - Aug 5, 2008 ...+ Au Canada, STOCRIN(R) est commercialisé par BMS sous le nom de SUSTIVA. << ---------------------- (1) Markowitz M, Nguyen BY, Gotuzzo E, et al. CNW Telbec (Communiqués de presse), Roche abandona la investigación en el campo del VIH - Jul 16, 2008 Entonces, la tendencia fue cambiar a los flamantes no análogos de nucleósido efavirenz (Sustiva®) y nevirapina (Viramune®). En marzo de 2003, Periodista Digital, Ardea Takes the More Exciting Route - Jun 26, 2008 This study could make or break RDEA806's future, because it will be tested head-to-head against the aforementioned Sustiva. If Sustiva significantly Motley Fool Ardea Biosciences Reports Additional Positive Phase 2a Results for ... - Jun 25, 2008 ...including those that are resistant to efavirenz (Sustiva(R)) and other currently available NNRTIs; a high genetic barrier to resistance; no reproductive Earthtimes (press release), Drugs Cut AIDS Deaths to Same Rates as Non-Patients (Update1) - Jul 1, 2008 Sustiva match those of uninfected people in the first five years after the virus takes hold, researchers said. The risk of death rises as the duration of Bloomberg Push for more HIV screens to drive Gilead's growth - Jun 27, 2008 ...s Sustiva. The combination pills make it easier for patients to comply with the drug "cocktail" regimen usually required by doctors. Forbes, CytoDyn Begins GMP Manufacturing of Its First-In-Class AIDS Drug - Jul 2, 2008 Several have been recently approved, including Sustiva(C) (efavirenz) from Bristol-Meyers Squibb (NYSE: BMY), and Rescriptor(C) (delavirdine) from Pfizer RedOrbit, The Top 60: Draftfcb Healthcare - Jun 30, 2008 ...for which the shop already handled US professional; BMS's HIV treatments Reyataz and Sustiva, along with immunosuppressant Belatacept, for transplants; Medical Marketing and Media, Macy's Celebrates Equal Marriage - Jun 23, 2008 Also that year, Grupo Campari's Skyy Vodka showed a woman on her knees proposing to another woman with a ring in a martini glass, and AIDS drug Sustiva 365Gay.com Boosted protease inhibitors have 60% lower risk of resistance ... - Jun 18, 2008 ...guidelines recommend that patients starting antiretroviral therapy for the first time should take a regimen based on the NNRTI efavirenz (Sustiva), Aidsmap, Nucleoside levels in seminal fluid higher than in blood, but not ... - Jun 18, 2008 ...nelfinavir (Viracept) and two indinavir (Crixivan)) and four took an NNRTI (three efavirenz (Sustiva), one nevirapine (Viramune)) alongside AZT/3TC. Aidsmap, Cambridge Who's Who Names Teresa M. Leezer Executive of the Year ... - Jun 18, 2008 Estimated launch product sales exceed $6 billion including worldwide blockbusters such as Fosamax, Zantac, Reyataz, Sustiva, Aleve and Rocephin. 24-7PressRelease.com (press release) Media advisory - ATRIPLA(TM) receives reimbursement approval in Quebec - 02 Jun 2008 ATRIPLA combines SUSTIVA(R) (efavirenz), manufactured by Bristol-Myers Squibb Company, and Truvada- (emtricitabine/tenofovir disoproxil fumarate), TMCnet Head-to-Head Trial Confirms Efavirenz (Sustiva) as Leader for ... - May 14, 2008 At the end of the 96-week randomized study, patients taking a combination of efavirenz (Sustiva) plus two nucleoside reverse transcriptase inhibitors MedPage Today, Ads blast Merck on AIDS drug prices in Mexico - May 30, 2008 The AIDS Healthcare Foundation launched a print ad aimed at shaming Merck in its own neighborhood for the prices it charges for AIDS drug Stocrin (Sustiva) Medical Marketing and Media, Gilead sees positive patent decision on Viread - May 21, 2008 ...(nyse: BMY - news - people )'s Sustiva. The remaining patents are still in effect while under review. In a note to investors, Lehman Brothers (nyse: LEH Forbes, Low rate of toxicity-related treatment change suggests HIV ... - May 28, 2008 The study found that some anti-HIV treatment combinations, for example those including tenofovir (Viread), efavirenz (Sustiva) or atazanavir (Reyataz) were Aidsmap, UPDATE 1-Gilead says US upholds one Viread patent - May 20, 2008 N: Quote, Profile, Research) Sustiva into a single pill. "We have always believed that the US PTO would recognize that Viread is a novel product, Reuters Does tenofovir increase the risk of efavirenz-associated liver ... - May 9, 2008 ...reported three cases which suggest that treatment with tenofovir (Viread) may increase the risk of liver side-effects caused by efavirenz (Sustiva). Aidsmap, Nearly all patients with NNRTI resistance could benefit from ... - May 8, 2008 But HIV can develop high-level cross-resistance to the two licensed NNRTIs (efavirenz, Sustiva and nevirapine, Viramune) after the emergence of a single Aidsmap, 'Shame on Merck': Drug Giant Blasted for Steep AIDS Drug Prices in ... - May 30, 2008 Merck's Stocrin (efavirenz, branded as Sustiva in the US), is a key component of many of the most effective antiretroviral AIDS drug therapy combinations. PharmaLive.com (press release), US study confirms long-term use of AZT, d4T result in lipoatrophy - May 27, 2008 ...and either a PI – most commonly nelfinavir (Viracept) or indinavir (Crixivan) – or one of the two NNRTIs, efavirenz (Sustiva) or nevirapine (Viramune). Aidsmap, Ardea Announces Progress With HIV Non-Nucleoside Reverse ... - May 23, 2008 ...range of HIV viral isolates, including those that are resistant to efavirenz (Sustiva(R), Bristol-Myers Squibb); a high genetic barrier to resistance; Medical News Today (press release), 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.
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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