Bexarotene

Bexarotene Brand Name– Targretin

What is Bexarotene

Bexarotene is a synthetic retinoid agent that activates retinoid X receptor (RXR) subtypes RXR-alpha, RXR-beta, and RXR-gamma.

Oral bexarotene is indicated for the treatment of cutaneous manifestations of cutaneous T-cell lymphoma (CTCL) in patients who are refractory to at least 1 prior systemic therapy.

Bexarotene gel is indicated for the topical treatment of cutaneous lesions in patients with stage IA and IB CTCL who have refractory or persistent disease after other therapies or who have not tolerated other therapies.

The FDA approved oral bexarotene in 1999; bexarotene gel received FDA approval in 2000.

Indications

1. breast cancer
2. cutaneous T-cell lymphoma (CTCL)
3. Kaposi’s sarcoma
4. mycosis fungoides
5. non-small cell lung cancer (NSCLC)
6. psoriasis

Side Effects

1. abdominal pain
2. acne vulgaris
3. agitation
4. alopecia
5. anemia
6. angina
7. anorexia
8. anorexia
9. arthralgia
10. asthenia
11. asthenia
12. ataxia
13. back pain
14. bleeding
15. blepharitis
16. bone pain
17. bullous rash
18. candidiasis
19. cataracts
20. cheilitis
21. chest pain (unspecified)
22. chills
23. cholestasis
24. coagulopathy
25. colitis
26. confusion
27. conjunctivitis
28. constipation
29. contact dermatitis
30. cough
31. depression
32. diarrhea
33. diarrhea
34. dizziness
35. dyspepsia
36. dyspnea
37. dysuria
38. edema
39. elevated hepatic enzymes
40. elevated hepatic enzymes
41. eosinophilia
42. erythema
43. exfoliative dermatitis
44. fever
45. flatulence
46. gingivitis
47. headache
48. headache
49. heart failure
50. hematuria
51. hemoptysis
52. hepatic failure
53. hyperamylasemia
54. hyperbilirubinemia
55. hyperbilirubinemia
56. hypercholesterolemia
57. hypercholesterolemia
58. hyperesthesia
59. hyperglycemia
60. hyperglycemia
61. hyperhidrosis
62. hyperkalemia
63. hyperlipidemia
64. hyperlipidemia
65. hypernatremia
66. hypertension
67. hypertriglyceridemia
68. hypertriglyceridemia
69. hypoalbuminemia
70. hypocalcemia
71. hypoesthesia
72. hyponatremia
73. hypothyroidism
74. hypothyroidism
75. hypoxia
76. infection
77. infection
78. influenza
79. insomnia
80. keratitis
81. leukopenia
82. leukopenia
83. lymphadenopathy
84. lymphocytosis
85. maculopapular rash
86. melena
87. myalgia
88. myasthenia
89. nausea
90. neutropenia
91. neutropenia
92. otalgia
93. pancreatitis
94. paresthesias
95. peripheral edema
96. peripheral edema
97. peripheral neuropathy
98. pharyngitis
99. photosensitivity
100. pleural effusion
101. pruritus
102. pulmonary edema
103. rash
104. rash
105. rhinitis
106. sinus tachycardia
107. skin irritation
108. skin ulcer
109. stroke
110. subdural hematoma
111. syncope
112. thrombocytopenia
113. urinary incontinence
114. urinary urgency
115. vesicular rash
116. visual impairment
117. vomiting
118. vomiting
119. weight gain
120. weight loss
121. xerophthalmia
122. xerosis
123. xerostomia

Monitoring Parameters

• CBC with differential
• LFTs
• pregnancy testing
• serum lipid profile
• thyroid function tests (TFTs)

Contraindications

• alcoholism
• biliary tract disease
• breast-feeding
• cataracts
• cholestasis
• contraception requirements
• diabetes mellitus
• hepatic disease
• hepatotoxicity
• hypercholesterolemia
• hyperlipidemia
• hypertriglyceridemia
• hypothyroidism
• leukopenia
• male-mediated teratogenicity
• neutropenia
• pancreatitis
• pregnancy
• pregnancy testing
• reproductive risk
• retinoid hypersensitivity
• sunlight (UV) exposure
• thyroid disease
• vaccination

Interactions

• Abacavir; Dolutegravir; Lamivudine
• Abemaciclib
• Acetaminophen; Butalbital; Caffeine; Codeine
• Acetaminophen; Caffeine; Dihydrocodeine
• Acetaminophen; Codeine
• Acetaminophen; Hydrocodone
• Acetaminophen; Oxycodone
• Acetohexamide
• Aliskiren; Amlodipine
• Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
• Alteplase
• Aminolevulinic Acid
• 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
• Antithymocyte Globulin
• Aprepitant, Fosaprepitant
• Aripiprazole
• Artemether; Lumefantrine
• Aspirin, ASA; Butalbital; Caffeine; Codeine
• Aspirin, ASA; Caffeine; Dihydrocodeine
• Aspirin, ASA; Carisoprodol; Codeine
• Aspirin, ASA; Oxycodone
• Atazanavir; Cobicistat
• Avapritinib
• Axitinib
• Bedaquiline
• Benzhydrocodone; Acetaminophen
• Brexpiprazole
• Brigatinib
• Bromocriptine
• Brompheniramine; Guaifenesin; Hydrocodone
• Brompheniramine; Hydrocodone; Pseudoephedrine
• Budesonide
• Budesonide; Formoterol
• Bupivacaine; Lidocaine
• Capmatinib
• Carbinoxamine; Hydrocodone; Phenylephrine
• Carbinoxamine; Hydrocodone; Pseudoephedrine
• Cariprazine
• Chlorpheniramine; Codeine
• Chlorpheniramine; Dihydrocodeine; Phenylephrine
• Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
• Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
• Chlorpheniramine; Hydrocodone
• Chlorpheniramine; Hydrocodone; Phenylephrine
• Chlorpheniramine; Hydrocodone; Pseudoephedrine
• Chlorpropamide
• Cholestyramine
• Clarithromycin
• Clozapine
• Cobicistat
• Cobimetinib
• Codeine
• Codeine; Guaifenesin
• Codeine; Phenylephrine; Promethazine
• Codeine; Promethazine
• Colestipol
• Conjugated Estrogens; Medroxyprogesterone
• Daclatasvir
• Dapsone
• Darunavir; Cobicistat
• Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
• Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
• Deflazacort
• Dexamethasone
• Dienogest; Estradiol valerate
• Digoxin
• Dihydrocodeine; Guaifenesin; Pseudoephedrine
• Diphenhydramine; Hydrocodone; Phenylephrine
• Diphenhydramine; Ibuprofen
• Diphenhydramine; Naproxen
• Dolutegravir
• Dolutegravir; Lamivudine
• Dolutegravir; Rilpivirine
• Doravirine
• Doravirine; Lamivudine; Tenofovir disoproxil fumarate
• Doxorubicin
• Dronabinol
• Dronedarone
• Drospirenone
• Drospirenone; Estradiol
• Drospirenone; Ethinyl Estradiol
• Drospirenone; Ethinyl Estradiol; Levomefolate
• Echinacea
• Elagolix; Estradiol; Norethindrone acetate
• Elbasvir; Grazoprevir
• Elexacaftor; tezacaftor; ivacaftor
• Elvitegravir
• Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
• Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
• Emtricitabine; Rilpivirine; Tenofovir alafenamide
• Emtricitabine; Rilpivirine; Tenofovir disoproxil fumarate
• Encorafenib
• Entrectinib
• Eravacycline
• Erdafitinib
• Erlotinib
• Esomeprazole; Naproxen
• Estradiol Cypionate; Medroxyprogesterone
• Estradiol; Levonorgestrel
• Estradiol; Norethindrone
• Estradiol; Norgestimate
• Estradiol; Progesterone
• Estrogens
• Ethinyl Estradiol; Desogestrel
• Ethinyl Estradiol; Ethynodiol Diacetate
• Ethinyl Estradiol; Etonogestrel
• Ethinyl Estradiol; Levonorgestrel
• Ethinyl Estradiol; Levonorgestrel; Ferrous bisglycinate
• Ethinyl Estradiol; Levonorgestrel; Folic Acid; Levomefolate
• Ethinyl Estradiol; Norelgestromin
• Ethinyl Estradiol; Norethindrone
• Ethinyl Estradiol; Norethindrone Acetate
• Ethinyl Estradiol; Norethindrone Acetate; Ferrous fumarate
• Ethinyl Estradiol; Norethindrone; Ferrous fumarate
• Ethinyl Estradiol; Norgestimate
• Ethinyl Estradiol; Norgestrel
• Etodolac
• Etonogestrel
• Famotidine; Ibuprofen
• Fedratinib
• Fenoprofen
• Filgrastim, G-CSF
• Flibanserin
• Flurbiprofen
• food
• Gemfibrozil
• Glasdegib
• Glimepiride
• Glimepiride; Pioglitazone
• Glimepiride; Rosiglitazone
• Glipizide
• Glipizide; Metformin
• Glyburide
• Glyburide; Metformin
• grapefruit juice
• Guaifenesin; Hydrocodone
• Guaifenesin; Hydrocodone; Pseudoephedrine
• Guanfacine
• Homatropine; Hydrocodone
• Hydrocodone
• Hydrocodone; Ibuprofen
• Hydrocodone; Phenylephrine
• Hydrocodone; Potassium Guaiacolsulfonate
• Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
• Hydrocodone; Pseudoephedrine
• Hydroxyprogesterone
• Ibrutinib
• Ibuprofen
• Ibuprofen; Oxycodone
• Ibuprofen; Pseudoephedrine
• Ifosfamide
• Indomethacin
• Insulins
• Isavuconazonium
• Ivabradine
• Ivacaftor
• Ixabepilone
• Ketoprofen
• Lansoprazole; Naproxen
• Lefamulin
• Lemborexant
• Leuprolide; Norethindrone
• Levonorgestrel
• Lidocaine
• Lidocaine; Prilocaine
• Live Vaccines
• Lopinavir; Ritonavir
• Lorlatinib
• Lumacaftor; Ivacaftor
• Lumateperone
• Lurasidone
• Lurbinectedin
• Maraviroc
• Meclofenamate Sodium
• Medroxyprogesterone
• Mefenamic Acid
• Meglitinides
• Meloxicam
• Mestranol; Norethindrone
• Methotrexate
• Methoxsalen
• Methylprednisolone
• Nabumetone
• Nanoparticle Albumin-Bound Paclitaxel
• Naproxen
• Naproxen; Pseudoephedrine
• Naproxen; Sumatriptan
• Neratinib
• Nisoldipine
• Norethindrone
• Norgestrel
• Olaparib
• Ombitasvir; Paritaprevir; Ritonavir
• Orlistat
• Oxaprozin
• Oxycodone
• Palifermin
• Pegfilgrastim
• Pemigatinib
• Penicillamine
• Perampanel
• Perindopril; Amlodipine
• Photosensitizing agents (topical)
• Pimavanserin
• Piroxicam
• Platelet Inhibitors
• Porfimer
• Praziquantel
• Prednisolone
• Prednisone
• Progesterone
• Progestins
• Reteplase, r-PA
• Rilpivirine
• Rimegepant
• Rofecoxib
• Roflumilast
• Romidepsin
• Ruxolitinib
• Salicylic Acid
• Segesterone Acetate; Ethinyl Estradiol
• Selpercatinib
• Selumetinib
• Simeprevir
• Siponimod
• Sodium Thiosulfate; Salicylic Acid
• Sofosbuvir; Velpatasvir
• Sofosbuvir; Velpatasvir; Voxilaprevir
• Sonidegib
• St. John’s Wort, Hypericum perforatum
• Streptokinase
• Sufentanil
• Sulfonylureas
• Sulindac
• Sunitinib
• Tasimelteon
• Tazemetostat
• Tbo-Filgrastim
• Telithromycin
• Tenecteplase
• Tetracyclines
• Tezacaftor; Ivacaftor
• Thiazolidinediones
• Thrombolytic Agents
• Tolazamide
• Tolbutamide
• Tolmetin
• Tolvaptan
• Triamcinolone
• Tuberculin Purified Protein Derivative, PPD
• Ubrogepant
• Ulipristal
• Urokinase
• Valdecoxib
• Venetoclax
• Verteporfin
• Vincristine
• Vincristine Liposomal
• Voxelotor
• Zanubrutinib
• Zolpidem