Rash as a side-effect of nelfinavir in children

Fortuny, Clàudia; Vicente, María Asunción; Medina, María Mercedes; González-Enseñat, A

doi:10.1097/00002030-200002180-00024

Cited by 19 publications

(5 citation statements)

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“…(2) The activity data should have a range of 4-5 orders of magnitude. (3) The compounds should be selected to provide clear and concise information and to avoid redundancy and bias in terms of both structural features and activity range. (4) The most active compounds should be included so that they provide information on most critical features required as a pharmacophore.…”

Section: Methodsmentioning

confidence: 99%

“…Although these drugs are helping to reduce the morbidity and mortality of HIV infection, their very high cost is prohibitive for most people infected in sub-Saharan Africa and third-world countries. Besides, these drugs have well documented side effects, − and development of resistance has been reported. − Therefore, discovery of new classes of potent and less-toxic anti-HIV-1 drugs with a different mechanism of action is urgently needed. The recent approval of a new class of drug, known as entry/fusion inhibitor T-20 (Fuzeone) − by the U.S. FDA, has generated hope that it might help infected people who are resistant to other available retroviral therapies.…”

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Generation of Predictive Pharmacophore Models for CCR5 Antagonists: Study with Piperidine- and Piperazine-Based Compounds as a New Class of HIV-1 Entry Inhibitors

Debnath

2003

J. Med. Chem.

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Predictive pharmacophore models were developed for a large series of piperidine- and piperazine-based CCR5 antagonists as anti-HIV-1 agents reported by Schering-Plough Research Institute in recent years. The pharmacophore models were generated using a training set consisting of 25 carefully selected antagonists based on well documented criteria. The activity spread, expressed in K(i), of training set molecules was from 0.1 to 1300 nM. The most predictive pharmacophore model (hypothesis 1), consisting of five features, namely, two hydrogen bond acceptors and three hydrophobic, had a correlation (r) of 0.920 and a root mean square of 0.879, and the cost difference between null cost and fixed cost was 44.46 bits. The model was cross-validated by randomizing the data using the CatScramble technique. The results confirmed that the pharmacophore models generated from the test set were not due to chance correlation. The best model (hypothesis 1) was validated using test set molecules (total of 78) and performed well in classifying active and inactive molecules correctly. The model was further validated by mapping onto it a diverse set of six CCR5 antagonists identified by five different pharmaceutical companies. The best model correctly predicted these compounds as being highly active. These multiple validation approaches provide confidence in the utility of the predictive pharmacophore model developed in this study as a 3D query tool in virtual screening to retrieve new chemical entities as potent CCR5 antagonists. The model can also be used in predicting biological activities of compounds prior to undertaking their costly synthesis.

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Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Generation of Predictive Pharmacophore Models for CCR5 Antagonists: Study with Piperidine- and Piperazine-Based Compounds as a New Class of HIV-1 Entry Inhibitors

Debnath

2003

J. Med. Chem.

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“…This rash was generally mild and was managed with prednisone and antihistamines while treatment was continued; no patients required the discontinuation of therapy. 81 A recent report also implicated nelfinavir as the precipitating factor in a case of porphyria cutanea tarda; the patient developed small white plaques, vesicles, and bullae on sun-exposed areas 3 days after commencing HAART. Urinary uroporphyrin levels were increased (2,083 mg per day).…”

Section: Other Protease Inhibitorsmentioning

confidence: 99%

Adverse Cutaneous Reactions to Antimicrobials in Patients with Human Immunodeficiency Virus Infection

Miller¹,

Warshaw²

2007

Dermatitis

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Adverse reactions to medication are significant contributors to morbidity and mortality in patients with human immunodeficiency virus (HIV) infection. Cutaneous events not only constitute a significant portion of these reactions, they may also herald developing systemic reactions such as hemato-, nephro-, and hepatotoxicity. The identification of cutaneous adverse reactions and drug culprits and the proper management of reactions are of paramount importance for these patients. This review focuses specifically on adverse cutaneous reactions to antimicrobials that are commonly used in the management of patients with HIV infection.

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“…Despite the fact that several new drugs were approved by the US FDA and these drugs are helping in reducing the morbidity and mortality of HIV infection, their very high cost is prohibitive for most people infected in Sub-Saharan Africa and third-world countries. Besides, these drugs have well documented side effects [2][3][4][5][6] and development of resistance has also been reported [7][8][9]. Therefore, a tremendous challenge is ahead in many different fronts to successfully combat this deadly disease.…”

Section: Introductionmentioning

confidence: 99%

Application of 3D-QSAR Techniques in Anti-HIV-1 Drug Design - An Overview

Debnath¹

2005

CPD

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Despite the availability of several classes of drugs against acquired immunodeficiency syndrome (AIDS) caused by human immunodeficiency virus type 1(HIV-1), this deadly disease showing very little sign of containment, especially in Sub-Saharan Africa and South-East Asia. More than 20 million people died since the first diagnosis of AIDS more than twenty years ago and almost 40 million people are currently living with HIV/AIDS. Structure-based drug design effort was immensely successful in identifying several drugs that are currently available for the treatment of HIV-1. Many applications have been reported on the use of quantitative structure-activity relationship (QSAR) studies to understand the drug-receptor interactions and help in the design of more effective analogs. Extensive application was also reported on the application of 3D-QSAR techniques, such as, Comparative Molecular Field Analysis (CoMFA), Comparative Molecular Similarity Analysis (CoMSIA), pharmacophore generation using Catalyst/HypoGen, free-energy binding analysis, GRID/GOLPE, HINT-based techniques, etc. in anti-HIV-1 drug discovery programs in academia and industry. We have attempted to put together a comprehensive overview on the 3D-QSAR applications in anti-HIV-1 drug design reported in the literature during the last decade.

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Rash as a side-effect of nelfinavir in children

Cited by 19 publications

References 1 publication

Generation of Predictive Pharmacophore Models for CCR5 Antagonists: Study with Piperidine- and Piperazine-Based Compounds as a New Class of HIV-1 Entry Inhibitors

Generation of Predictive Pharmacophore Models for CCR5 Antagonists: Study with Piperidine- and Piperazine-Based Compounds as a New Class of HIV-1 Entry Inhibitors

Adverse Cutaneous Reactions to Antimicrobials in Patients with Human Immunodeficiency Virus Infection

Application of 3D-QSAR Techniques in Anti-HIV-1 Drug Design - An Overview

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