Maraviroc

Maraviroc Brand Name– Selzentry

What is Maraviroc

Maraviroc is an antiretroviral agent indicated for the treatment of CCR5-tropic HIV. It was the first antiretroviral approved that blocked HIV entry into human cells via its predominant entry route, the CCR5 co-receptor.

There are 2 co-receptors that allow HIV entry into CD4 cells: CCR5 and CXCR4.

Maraviroc is only effective at reducing viral load in patients with CCR5-tropic HIV strains; it is not effective against virus targeting the CXCR4 co-receptor (i.e., CXCR4-tropic HIV) and has a limited effect against virus with the ability to target both receptors (i.e., dual-tropic HIV).

CXCR4-tropic and dual-tropic HIV strains are common in patients who have been infected with HIV for several years therefore, a tropism assay of the HIV strain is necessary prior to treatment.

Hepatotoxicity has been reported with use of maraviroc and may be accompanied by signs or symptoms of a systemic allergic reaction. In clinical trials, adult patients who were at increased risk of cardiovascular events experienced such events including myocardial ischemia and infarction.

Maraviroc is a substrate of CYP3A and dosing is reliant upon concurrently administered drugs.

Maraviroc was granted accelerated conditional approval by the FDA in August 2007, and full approval in November 2008 for treatment-experienced adults.

The FDA approved maraviroc for use in treatment-naive adults in November 2009; it was approved in pediatric patients 2 years and older weighing at least 10 kg in November 2016

Indications

  1. human immunodeficiency virus (HIV)
  2. human immunodeficiency virus (HIV) infection
  3. human immunodeficiency virus (HIV) prophylaxis

NOTE: Maraviroc must ONLY be used in patients with CCR5-tropic HIV infection. Tropism testing conducted on a current sample should guide treatment; do not use in patients with dual or CXCR4-tropic HIV, as efficacy was not demonstrated in a phase 2 study of this patient group.

NOTE: As compared to treatment with efavirenz, treatment-naive adults treated with maraviroc experienced more virologic failure and lamivudine resistance.

Side Effects

  1. abdominal pain
  2. acne vulgaris
  3. alopecia
  4. anemia
  5. angina
  6. anxiety
  7. arthralgia
  8. candidiasis
  9. cirrhosis
  10. conjunctivitis
  11. constipation
  12. cough
  13. Cushingoid features
  14. depression
  15. diarrhea
  16. dizziness
  17. Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)
  18. dysesthesia
  19. dyspnea
  20. edema
  21. ejaculation dysfunction
  22. elevated hepatic enzymes
  23. eosinophilia
  24. erythema
  25. fever
  26. flatulence
  27. folliculitis
  28. gynecomastia
  29. heart failure
  30. hepatic failure
  31. hepatitis
  32. hepatotoxicity
  33. hyperamylasemia
  34. hyperbilirubinemia
  35. hypertension
  36. infection
  37. influenza
  38. insomnia
  39. jaundice
  40. lipodystrophy
  41. memory impairment
  42. meningitis
  43. myalgia
  44. myocardial infarction
  45. nasal congestion
  46. nausea
  47. neutropenia
  48. new primary malignancy
  49. ocular infection
  50. orthostatic hypotension
  51. osteonecrosis
  52. paresthesias
  53. peripheral neuropathy
  54. pruritus
  55. pseudomembranous colitis
  56. rash
  57. rhabdomyolysis
  58. rhinitis
  59. seizures
  60. sinusitis
  61. Stevens-Johnson syndrome
  62. stroke
  63. syncope
  64. thrombosis
  65. toxic epidermal necrolysis
  66. tremor
  67. visual impairment
  68. vomiting

Monitoring Parameters

  • blood glucose
  • CBC with differential
  • CD4+ T cell count
  • hepatitis B serology
  • LFTs
  • plasma hepatitis C RNA
  • plasma HIV RNA
  • pregnancy testing
  • serum bilirubin (total and direct)
  • serum cholesterol
  • serum creatinine
  • serum lipid profile
  • urinalysis

Contraindications

  • Asian patients
  • autoimmune disease
  • breast-feeding
  • cardiac disease
  • children
  • dialysis
  • fever
  • geriatric
  • Graves’ disease
  • Guillain-Barre syndrome
  • hepatic disease
  • hepatitis
  • hepatitis B and HIV coinfection
  • hepatitis C and HIV coinfection
  • hepatotoxicity
  • human immunodeficiency virus (HIV) infection resistance
  • immune reconstitution syndrome
  • infants
  • infection
  • myocardial infarction
  • neonates
  • orthostatic hypotension
  • pregnancy
  • renal failure
  • renal impairment
  • serious rash

Interactions

  • Acetaminophen; Propoxyphene
  • Adefovir
  • Aldesleukin, IL-2
  • Aliskiren; Amlodipine
  • Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
  • Amiodarone
  • Amlodipine
  • Amlodipine; Atorvastatin
  • Amlodipine; Benazepril
  • Amlodipine; Celecoxib
  • Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
  • Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
  • Amlodipine; Olmesartan
  • Amlodipine; Telmisartan
  • Amlodipine; Valsartan
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Amprenavir
  • Apalutamide
  • Aprepitant, Fosaprepitant
  • Armodafinil
  • Atazanavir
  • Atazanavir; Cobicistat
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Bexarotene
  • Boceprevir
  • Brigatinib
  • Cabozantinib
  • Capmatinib
  • Carbamazepine
  • Carvedilol
  • Ceritinib
  • Chloramphenicol
  • Cidofovir
  • Cimetidine
  • Ciprofloxacin
  • Clarithromycin
  • Clobazam
  • Cobicistat
  • Colchicine; Probenecid
  • Conivaptan
  • Cyclosporine
  • Dabrafenib
  • Daclatasvir
  • Danazol
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Deferasirox
  • Delavirdine
  • Dexamethasone
  • Dextromethorphan; Quinidine
  • Diltiazem
  • Dronedarone
  • Duvelisib
  • Efavirenz
  • Efavirenz; Emtricitabine; Tenofovir
  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Elbasvir; Grazoprevir
  • Elexacaftor; tezacaftor; ivacaftor
  • Eliglustat
  • Eltrombopag
  • Elvitegravir
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Encorafenib
  • Enzalutamide
  • Erythromycin
  • Erythromycin; Sulfisoxazole
  • Eslicarbazepine
  • Ethanol
  • Etravirine
  • Felbamate
  • Flibanserin
  • Fluconazole
  • Fluoxetine
  • Fluoxetine; Olanzapine
  • Flutamide
  • Fosamprenavir
  • Fosphenytoin
  • Fostamatinib
  • Furosemide
  • Gemfibrozil
  • Glecaprevir; Pibrentasvir
  • grapefruit juice
  • Idelalisib
  • Imatinib
  • Indinavir
  • Isavuconazonium
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Itraconazole
  • Ivacaftor
  • Ixabepilone
  • Ketoconazole
  • Lapatinib
  • Ledipasvir; Sofosbuvir
  • Leflunomide
  • Lesinurad
  • Lesinurad; Allopurinol
  • Letermovir
  • Lomitapide
  • Lopinavir; Ritonavir
  • Lorlatinib
  • Lumacaftor; Ivacaftor
  • Lumacaftor; Ivacaftor
  • Mefloquine
  • Mifepristone
  • Mitotane
  • Modafinil
  • Nafcillin
  • Nefazodone
  • Nelfinavir
  • Neratinib
  • Netupitant, Fosnetupitant; Palonosetron
  • Nicardipine
  • Nifedipine
  • Obeticholic Acid
  • Octreotide
  • Ombitasvir; Paritaprevir; Ritonavir
  • Omeprazole; Amoxicillin; Rifabutin
  • Oritavancin
  • Osimertinib
  • Oxcarbazepine
  • Pazopanib
  • Perampanel
  • Perindopril; Amlodipine
  • Phenobarbital
  • Phentermine; Topiramate
  • Phenytoin
  • Pirfenidone
  • Ponatinib
  • Posaconazole
  • Primidone
  • Probenecid
  • Propafenone
  • Propoxyphene
  • Quinidine
  • Quinine
  • Ranolazine
  • Ribociclib
  • Ribociclib; Letrozole
  • Rifabutin
  • Rifampin
  • Rifapentine
  • Rifaximin
  • Ritonavir
  • Rolapitant
  • Sapropterin
  • Saquinavir
  • Simeprevir
  • Sofosbuvir; Velpatasvir
  • Sofosbuvir; Velpatasvir; Voxilaprevir
  • Sorafenib
  • St. John’s Wort, Hypericum perforatum
  • Tacrolimus
  • Telaprevir
  • Telithromycin
  • Telotristat Ethyl
  • Temsirolimus
  • Teriflunomide
  • Testosterone
  • Tezacaftor; Ivacaftor
  • Ticagrelor
  • Topiramate
  • Trandolapril; Verapamil
  • Tucatinib
  • Valproic Acid, Divalproex Sodium
  • Vemurafenib
  • Verapamil
  • Voriconazole
  • Zafirlukast
  • Zonisamide
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