Maraviroc

Brand names: Selzentry™

Drug Forms:
• Maraviroc Oral Tablets (below)
• Maraviroc Oral tablet

Español:
• Maraviroc, Tableta oral

Maraviroc Oral Tablets

What are Maraviroc Oral Tablets?

Maraviroc is an antiretroviral drug. It is used with other medicines to treat some strains of HIV. This medicine is not a cure for HIV. It will not stop the spread of HIV to others.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• heart disease or high risk of heart disease
• hepatitis B or C
• kidney disease
• liver disease
• low blood pressure or take medicines to lower blood pressure
• an unusual or allergic reaction to maraviroc, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should this medicine be used?

Take this medicine by mouth. Follow the directions on the prescription label. Do not cut, crush or chew this medicine. You can take it with or without food. If it upsets your stomach, take it with food. Take your medicine at regular intervals. Do not take your medicine more often than directed. For your anti-HIV therapy to work as well as possible, take each dose exactly as prescribed. Do not skip doses or stop your medicine even if you feel better. Skipping doses may make the HIV virus resistant to this medicine and other medicines. Do not stop taking except on your doctor's advice.

A patient information sheet for the product will be given with each prescription and refill. Read this sheet carefully each time. The sheet may change frequently.

A special MedGuide will be given to you by the pharmacist with each prescription and refill. Be sure to read this information carefully each time.

Talk to your pediatrician regarding the use of this medicine in children. This medicine is not approved for use in children.

What drug(s) may interact with Maraviroc?

• clarithromycin
• medicines for fungal infections like ketoconazole, itraconazole
• medicines for seizures like carbamazepine, phenobarbital, phenytoin
• nefazadone
• other medicines for HIV like darunavir, delavirdine, efavirenz, indinavir, ritonavir
• rifampin
• St. John's Wort

Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking Maraviroc?

Visit your doctor or health care professional for regular check ups. Discuss any new symptoms with your doctor. You will need to have important blood work done while on this medicine.

HIV is spread to others through sexual or blood contact. Talk to your doctor about how to stop the spread of HIV.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells.

What side effects may I notice from receiving Maraviroc?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
• breathing problems
• chest pain
• dark urine
• feeling faint or lightheaded, falls
• fever, infection, flu-like symptoms
• right upper belly pain
• tingling, pain or numbness in the hands or feet
• trouble passing urine or change in the amount of urine
• unusually tired or weak
• vomiting
• yellowing of the eyes or skin

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• aches, pains
• cough
• diarrhea
• dizziness
• trouble sleeping

Where can I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Throw away any unused medicine after the expiration date.

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

Maraviroc
Systematic (IUPAC) name
4,4-difluoro-N-{(1S)-3-[3-(3-isopropyl- 5-methyl-4H-1,2,4-triazol-4-yl)- 8-azabicyclo[3.2.1]oct-8-yl]-1- phenylpropyl}cyclohexanecarboxamide
Identifiers
CAS number	376348-65-1
ATC code	J05AX09
PubChem	3002977
Chemical data
Formula	C29H41F2N5O
Mol. mass	513.666 g/mol
Pharmacokinetic data
Bioavailability	23% [1]
Metabolism	?
Half life	16 h [2]
Excretion	?
Therapeutic considerations
Licence data	EU EMEA:link, US FDA:link
Pregnancy cat.	B(US)
Legal status	POM(UK) ℞-only(US)
Routes	Oral
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Maraviroc (brand-named Selzentry, or Celsentri outside the U.S.) is a drug used in the treatment of HIV infection.

Contents 1 Mechanism of action 2 Development and approval 3 Efficacy 4 Safety 5 See also 6 References 7 External links

Mechanism of action

Maraviroc is an entry inhibitor. Specifically, maraviroc blocks the chemokine receptor CCR5 which HIV uses as a coreceptor to bind and enter a human macrophage^[3]. Because HIV can also use another coreceptor, CXCR4, an HIV tropism test such as a trofile assay must be performed to determine if the drug will be effective.^[4]

Development and approval

Maraviroc, originally designated UK-427857, was developed by the drug company Pfizer in its UK labs located in Sandwich. On April 24, 2007 the U.S. Food and Drug Administration advisory panel reviewing maraviroc's New Drug Application unanimously recommended approval for the new drug,^[5] and the drug received full FDA approval on August 6, 2007 for use in treatment experienced patients.^[6]

On September 24, 2007, Pfizer announced that the European Commission approved Maraviroc. Industry experts forecast annual Maraviroc sales of $500 million by 2011.^[7]

Efficacy

Two randomized, placebo-controlled clinical trials, known as MOTIVATE 1 & 2, compared 209 patients receiving optimized therapy plus a placebo to 426 patients receiving optimized therapy plus 150 mg maraviroc once daily and 414 patients receiving optimized therapy plus 150 mg maraviroc twice daily. At 48 weeks, 55% of participants receiving maraviroc once daily and 60% of participants receiving the drug twice daily achieved a viral load of less than 400 copies/mL compared with 26% of those taking placebo; about 44% of the once-daily and 45% of the twice-daily maraviroc group had a viral load of less than 50 copies/mL compared with about 23% of those who received placebo. In addition, those who received the entry inhibitor had a mean increase in CD4 cells of 110 cells/µL in the once-daily group, 106 cells/µL in the twice-daily group, and 56 cells/µL in the placebo group.^[8][9][10]

Safety

The MOTIVATE trials showed no clinically relevant differences in safety between the maraviroc and placebo groups. However, researchers question the long-term safety of blocking CCR5, a receptor whose function in the healthy individual is not fully understood.^[8]

See also

• Discovery and development of CCR5 receptor antagonists

References

1. ^ Abel S, Russell D, Whitlock LA, Ridgway CE, Nedderman AN, Walker DK. (2008). "Assessment of the absorption, metabolism and absolute bioavailability of maraviroc in healthy male subjects.". Br J Clin Pharmacol. 65 (1): 60-7. PMID 18333867. http://www.ncbi.nlm.nih.gov/pubmed/18333867?ordinalpos=20&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsPanel.Pubmed_DefaultReportPanel.Pubmed_RVDocSum. 
2. ^ Abel S, Back DJ, Vourvahis M. (2009). "Maraviroc: pharmacokinetics and drug interactions.". Antivir Ther. 14 (5): 607-18. PMID 19704163. http://www.ncbi.nlm.nih.gov/pubmed/19704163?ordinalpos=4&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsPanel.Pubmed_DefaultReportPanel.Pubmed_RVDocSum. 
3. ^ "HIV pathogenesis: 25 years of progess and persitent challenges" Jay A. Levy, AIDS 2009 (23) : 147-160
4. ^ Biswas P, Tambussi G, Lazzarin A (2007). "Access denied? The status of co-receptor inhibition to counter HIV entry". Expert Opin Pharmacother 8 (7): 923–33. doi:10.1517/14656566.8.7.923. PMID 17472538. http://www.expertopin.com/doi/abs/10.1517/14656566.8.7.923. 
5. ^ Gay News From 365Gay.com
6. ^ "Pfizer wins U.S. approval for new HIV drug". http://www.reuters.com/article/ousiv/idUSN0642522320070806. Retrieved 2007-08-06. 
7. ^ Reuters, Europe gives final approval to Pfizer HIV drug
8. ^ ^{a b} Stephenson J (2007). "Researchers buoyed by novel HIV drugs: will expand drug arsenal against resistant virus". JAMA 297 (14): 1535–6. doi:10.1001/jama.297.14.1535. PMID 17426263. http://jama.ama-assn.org/cgi/pmidlookup?view=long&pmid=17426263. 
9. ^ Emmelkamp JM, Rockstroh JK (2007). "CCR5 antagonists: comparison of efficacy, side effects, pharmacokinetics and interactions--review of the literature". Eur. J. Med. Res. 12 (9): 409–17. PMID 17933722. 
10. ^ "Maraviroc reduces viral load in naive patients at 48 weeks". AIDS Patient Care STDS 21 (9): 703–4. 2007. PMID 17941136. 

External links

• BBC News story: Drug 'stops HIV's entry to cells'
• Maraviroc data at aidsmap
• Maraviroc early access program
• New HIV Drug Recommended for Approval
• MeSH maraviroc

v • d • e Antiviral drugs: antiretroviral drugs used against HIV (primarily J05) Entry/fusion inhibitors (Discovery & development) gp41 (Enfuvirtide) · CCR5 (Maraviroc, Vicriviroc†, PRO 140†) · CD4 (Ibalizumab†) Reverse transcriptase inhibitors (RTIs) Nucleoside & Nucleotide (NRTI) Nucleoside analogues/NARTIs: Abacavir (ABC)°# · Emtricitabine (FTC)°# · Lamivudine (3TC)°# · Didanosine (ddI)# · Zidovudine (AZT)# · Apricitabine† · Stampidine† · Elvucitabine† · Racivir† · Amdoxovir† · Stavudine (d4T)# · Zalcitabine (ddC)◊ Nucleotide analogues/NtRTIs: Tenofovir°# Non-Nucleoside (NNRTI) (Discovery & development) (1st gen) Efavirenz°# · Nevirapine#  · Loviride◊ · Delavirdine◊ · (2nd gen) diarylpyrimidines (Etravirine, Rilpivirine†)  · Lersivirine† Integrase inhibitors Raltegravir · Elvitegravir† · Globoidnan A (experimental)  · MK-2048† Maturation inhibitors Bevirimat† · Vivecon† Protease Inhibitors (PI) (Discovery & development) Atazanavir° · Fosamprenavir° · Lopinavir°# · Darunavir · Nelfinavir# · Ritonavir# · Saquinavir# · Tipranavir · Amprenavir◊ · Indinavir◊# Combined formulations Combivir · Atripla · Trizivir · Truvada · Kaletra · Epzicom Experimental agents Uncoating inhibitors TRIM5alpha (gene) Transcription inhibitors Tat antagonists Translation inhibitors Trichosanthin Other Abzyme · Calanolide A · Ceragenin · Cyanovirin-N · Diarylpyrimidines · Epigallocatechin gallate (EGCG) · Foscarnet · Griffithsin · Hydroxyurea · Miltefosine · Portmanteau inhibitors · Seliciclib† · Synergistic enhancers · Tre recombinase · Zinc finger protein transcription factor · KP-1461† Failed agents Dexelvucitabine · Capravirine · Emivirine · Lodenosine · Atevirdine · Brecanavir · Aplaviroc #WHO-EM. ‡Withdrawn from market. CLINICAL TRIALS: †Phase III. §Never to phase III °DHHS preferred first-line agent. ◊Formerly or rarely used agent.

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