Everolimus

Everolimus Brand Names- Afinitor | Afinitor DISPERZ | Zortress

What is Everolimus

Everolimus is a macrolide immunosuppressant and analog of sirolimus that inhibits mammalian target of rapamycin (mTOR), a serine-threonine kinase, downstream of the PI3K/AKT pathway.

The mTOR pathway is dysregulated in many human cancers and in tuberous sclerosis complex (TSC). Inhibition of mTOR has been shown to reduce cell proliferation, angiogenesis, and glucose uptake by the tumor.

Everolimus (Afinitor or Afinitor Disperz) is indicated for the treatment of certain patients with advanced breast cancer, pancreatic neuroendocrine tumors (PNET), neuroendocrine tumors (NET) of GI or lung origin, renal cell cancer, and TSC-associated conditions including renal angiomyolipoma, subependymal giant cell astrocytoma (SEGA), and partial-onset seizures.

Everolimus also inhibits antigenic and interleukin (IL-2 and IL-15) stimulated activation and proliferation of T and B lymphocytes, and under the brand name, Zortress is indicated for the prophylaxis of organ rejection in certain patients after either kidney or liver transplantation.

Zortress carries black box warnings for increased susceptibility to infection and the possible development of immunosuppression-related malignancies (e.g., lymphoma and skin cancer), increased risk of kidney graft thrombosis within 30 days post-transplant, nephrotoxicity with the use of standard-exposure cyclosporine, and increased mortality in patients after heart transplantation. Use everolimus with caution in the peri-surgical period due to the risk of impaired wound healing.

Indications

1. astrocytoma
2. breast cancer
3. carcinoid
4. kidney transplant rejection prophylaxis
5. liver transplant rejection prophylaxis
6. macroglobulinemia
7. malignant neuroendocrine tumor (NET)
8. partial seizures
9. renal angiomyolipoma
10. renal cell cancer

For the treatment of patients with advanced renal cell cancer (RCC)

for the treatment of patients with advanced renal cell cancer who have failed treatment with sunitinib or sorafenib

Side Effects

1. abdominal pain
2. abdominal pain
3. acne vulgaris
4. acneiform rash
5. agitation
6. agitation
7. alopecia
8. amenorrhea
9. anaphylactoid reactions
10. anemia
11. anemia
12. angina
13. angioedema
14. anorexia
15. anorexia
16. anxiety
17. anxiety
18. arthralgia
19. arthralgia
20. ascites
21. asthenia
22. asthenia
23. atrial fibrillation
24. azoospermia
25. back pain
26. back pain
27. BK virus-associated nephropathy
28. bladder spasm
29. bleeding
30. blurred vision
31. candidiasis
32. cataracts
33. chest pain (unspecified)
34. chills
35. cholangitis
36. cholestasis
37. colitis
38. conjunctivitis
39. constipation
40. constipation
41. cough
42. cough
43. Cushingoid features
44. dehydration
45. depression
46. diabetes mellitus
47. diabetes mellitus
48. diarrhea
49. diarrhea
50. dizziness
51. dizziness
52. dysgeusia
53. dysgeusia
54. dysmenorrhea
55. dyspepsia
56. dysphagia
57. dyspnea
58. dyspnea
59. dysuria
60. edema
61. elevated hepatic enzymes
62. elevated hepatic enzymes
63. enterocolitis
64. epistaxis
65. epistaxis
66. erythema
67. exfoliative dermatitis
68. fatigue
69. fatigue
70. fever
71. fever
72. flatulence
73. fluid retention
74. flushing
75. folliculitis
76. gastritis
77. gastroesophageal reflux
78. gingival hyperplasia
79. glossitis
80. gout
81. hallucinations
82. headache
83. headache
84. heart failure
85. hematoma
86. hematuria
87. hemolytic-uremic syndrome
88. hemorrhoids
89. hepatitis
90. hirsutism
91. hyperbilirubinemia
92. hyperbilirubinemia
93. hypercalcemia
94. hypercholesterolemia
95. hypercholesterolemia
96. hyperglycemia
97. hyperglycemia
98. hyperkalemia
99. hyperlipidemia
100. hypertension
101. hypertension
102. hypertensive crisis
103. hypertrichosis
104. hypertriglyceridemia
105. hypertriglyceridemia
106. hyperuricemia
107. hypoalbuminemia
108. hypoalbuminemia
109. hypocalcemia
110. hypocalcemia
111. hypoesthesia
112. hypoglycemia
113. hypokalemia
114. hypokalemia
115. hypomagnesemia
116. hyponatremia
117. hyponatremia
118. hypophosphatemia
119. hypophosphatemia
120. hypotension
121. hypothyroidism
122. ileus
123. immunosuppression
124. impaired wound healing
125. impotence (erectile dysfunction)
126. infection
127. infection
128. infertility
129. influenza
130. insomnia
131. insomnia
132. interstitial lung disease
133. interstitial lung disease
134. interstitial nephritis
135. iron deficiency
136. lethargy
137. leukocytosis
138. leukoencephalopathy
139. leukopenia
140. leukopenia
141. lymphadenopathy
142. lymphocele
143. lymphopenia
144. lymphopenia
145. maculopapular rash
146. malaise
147. menorrhagia
148. menstrual irregularity
149. metabolic acidosis
150. migraine
151. musculoskeletal pain
152. myalgia
153. myocarditis
154. nasal congestion
155. nausea
156. nausea
157. nephrotoxicity
158. neutropenia
159. neutropenia
160. new primary malignancy
161. nocturia
162. oligospermia
163. oral ulceration
164. osteomyelitis
165. osteonecrosis
166. osteopenia
167. osteoporosis
168. palmar-plantar erythrodysesthesia (hand and foot syndrome)
169. palpitations
170. pancreatitis
171. pancytopenia
172. paresis
173. paresthesias
174. pericardial effusion
175. peripheral edema
176. peripheral edema
177. pharyngitis
178. phlebitis
179. pleural effusion
180. pneumonitis
181. pneumonitis
182. polyuria
183. prolonged bleeding time
184. prolonged bleeding time
185. prostatic hypertrophy
186. proteinuria
187. proteinuria
188. pruritus
189. pruritus
190. pulmonary edema
191. pulmonary embolism
192. pulmonary fibrosis
193. pulmonary hypertension
194. pyuria
195. rash
196. rash
197. renal failure (unspecified)
198. renal graft thrombosis
199. renal tubular necrosis
200. rhinorrhea
201. sinus tachycardia
202. sinusitis
203. steatorrhea
204. stomatitis
205. stomatitis
206. syncope
207. thrombocytopenia
208. thrombocytopenia
209. thrombocytosis
210. thromboembolism
211. thrombosis
212. thrombotic microangiopathy
213. thrombotic thrombocytopenic purpura (TTP)
214. urinary retention
215. urinary urgency
216. urticaria
217. vaginal bleeding
218. vasculitis
219. vitamin B12 deficiency
220. vomiting
221. vomiting
222. weakness
223. weight loss
224. weight loss
225. wheezing
226. wound dehiscence
227. xerosis
228. xerosis
229. xerostomia

Monitoring Parameters

• blood glucose
• CBC with differential
• LFTs
• pregnancy testing
• serum bilirubin
• serum creatinine
• serum lipid profile
• serum triglycerides
• skin cancer screening exam
• urinalysis

Contraindications

• angioedema
• bone marrow suppression
• breast-feeding
• contraception requirements
• diabetes mellitus
• fungal infection
• geriatric
• heart transplant
• hypercholesterolemia
• hyperglycemia
• hyperlipidemia
• hypertriglyceridemia
• immunosuppression
• impaired wound healing
• infection
• infertility
• interstitial lung disease
• lactase deficiency
• lymphoma
• mortality
• nephrotoxicity
• new primary malignancy
• pneumonitis
• pregnancy
• pregnancy testing
• proteinuria
• renal artery thrombosis
• renal disease
• renal graft thrombosis
• renal impairment
• renal vein thrombosis
• reproductive risk
• skin cancer
• stomatitis
• sunlight (UV) exposure
• surgery
• vaccination
• wound dehiscence

Interactions

• Acetaminophen; Butalbital; Caffeine; Codeine
• Acetaminophen; Caffeine; Dihydrocodeine
• Acetaminophen; Codeine
• Acetaminophen; Hydrocodone
• Acetaminophen; Oxycodone
• Acetaminophen; Tramadol
• Alfentanil
• Aliskiren; Amlodipine
• Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
• Amiodarone
• Amitriptyline
• Amitriptyline; Chlordiazepoxide
• Amlodipine
• Amlodipine; Atorvastatin
• Amlodipine; Benazepril
• Amlodipine; Celecoxib
• Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
• Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
• Amlodipine; Olmesartan
• Amlodipine; Telmisartan
• Amlodipine; Valsartan
• Amoxapine
• Amoxicillin; Clarithromycin; Lansoprazole
• Amoxicillin; Clarithromycin; Omeprazole
• Angiotensin-converting enzyme inhibitors
• Apalutamide
• Aprepitant, Fosaprepitant
• Aspirin, ASA; Butalbital; Caffeine; Codeine
• Aspirin, ASA; Caffeine; Dihydrocodeine
• Aspirin, ASA; Carisoprodol; Codeine
• Aspirin, ASA; Oxycodone
• Aspirin, ASA; Pravastatin
• Atazanavir
• Atazanavir; Cobicistat
• Atorvastatin
• Atorvastatin; Ezetimibe
• Atropine; Hyoscyamine; Phenobarbital; Scopolamine
• Belladonna Alkaloids; Ergotamine; Phenobarbital
• Benazepril
• Benazepril; Hydrochlorothiazide, HCTZ
• Benzhydrocodone; Acetaminophen
• Brigatinib
• Brompheniramine; Guaifenesin; Hydrocodone
• Brompheniramine; Hydrocodone; Pseudoephedrine
• Cabozantinib
• Caffeine; Ergotamine
• Canakinumab
• Capmatinib
• Captopril
• Captopril; Hydrochlorothiazide, HCTZ
• Carbamazepine
• Carbinoxamine; Hydrocodone; Phenylephrine
• Carbinoxamine; Hydrocodone; Pseudoephedrine
• Ceritinib
• Chloramphenicol
• Chlorpheniramine; Codeine
• Chlorpheniramine; Dihydrocodeine; Phenylephrine
• Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
• Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
• Chlorpheniramine; Hydrocodone
• Chlorpheniramine; Hydrocodone; Phenylephrine
• Chlorpheniramine; Hydrocodone; Pseudoephedrine
• Ciprofloxacin
• Clarithromycin
• Clofazimine
• Clomipramine
• Clozapine
• Cobicistat
• Codeine
• Codeine; Guaifenesin
• Codeine; Phenylephrine; Promethazine
• Codeine; Promethazine
• Colchicine
• Colchicine; Probenecid
• Conivaptan
• Crizotinib
• Cyclosporine
• Daclatasvir
• Danazol
• Darunavir
• Darunavir; Cobicistat
• Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
• Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
• Delavirdine
• Desipramine
• Dextromethorphan; Quinidine
• Dihydrocodeine; Guaifenesin; Pseudoephedrine
• Dihydroergotamine
• Diltiazem
• Diphenhydramine; Hydrocodone; Phenylephrine
• Disopyramide
• Dofetilide
• Doxepin
• Dutasteride; Tamsulosin
• Duvelisib
• Echinacea
• Efavirenz
• Efavirenz; Emtricitabine; Tenofovir
• Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
• Elexacaftor; tezacaftor; ivacaftor
• Eliglustat
• Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
• Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
• Emapalumab
• Enalapril, Enalaprilat
• Enalapril; Felodipine
• Enalapril; Hydrochlorothiazide, HCTZ
• Encorafenib
• Enzalutamide
• Erdafitinib
• Ergotamine
• Erythromycin
• Erythromycin; Sulfisoxazole
• Ethosuximide
• Ezetimibe; Simvastatin
• Fedratinib
• Fentanyl
• Flecainide
• Flibanserin
• Fluconazole
• Fluoxetine
• Fluoxetine; Olanzapine
• Fluvastatin
• Fluvoxamine
• Fosamprenavir
• Fosinopril
• Fosinopril; Hydrochlorothiazide, HCTZ
• Fosphenytoin
• Fostamatinib
• grapefruit juice
• Guaifenesin; Hydrocodone
• Guaifenesin; Hydrocodone; Pseudoephedrine
• Haloperidol
• Homatropine; Hydrocodone
• Hydrochlorothiazide, HCTZ; Lisinopril
• Hydrochlorothiazide, HCTZ; Moexipril
• Hydrochlorothiazide, HCTZ; Quinapril
• Hydrocodone
• Hydrocodone; Ibuprofen
• Hydrocodone; Phenylephrine
• Hydrocodone; Potassium Guaiacolsulfonate
• Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
• Hydrocodone; Pseudoephedrine
• Ibuprofen; Oxycodone
• Idelalisib
• Imatinib
• Imipramine
• Indinavir
• Isoniazid, INH; Pyrazinamide, PZA; Rifampin
• Isoniazid, INH; Rifampin
• Isradipine
• Istradefylline
• Itraconazole
• Ivacaftor
• Ivosidenib
• Ixabepilone
• Ketoconazole
• Lanreotide
• Lapatinib
• Lasmiditan
• Lefamulin
• Lemborexant
• Letermovir
• Lisinopril
• Live Vaccines
• Lomitapide
• Lopinavir; Ritonavir
• Lovastatin
• Lovastatin; Niacin
• Lumacaftor; Ivacaftor
• Lumacaftor; Ivacaftor
• Maprotiline
• Mefloquine
• Mephobarbital
• Methadone
• Midazolam
• Mifepristone
• Mitotane
• Moexipril
• Natalizumab
• Nefazodone
• Nelfinavir
• Niacin; Simvastatin
• Nimodipine
• Nisoldipine
• Nortriptyline
• Octreotide
• Ombitasvir; Paritaprevir; Ritonavir
• Oxycodone
• Palifermin
• Penicillamine
• Perindopril
• Perindopril; Amlodipine
• Perphenazine; Amitriptyline
• Phenobarbital
• Phenytoin
• Pimozide
• Pitavastatin
• Ponatinib
• Posaconazole
• Pravastatin
• Primidone
• Propafenone
• Protriptyline
• Quinapril
• Quinidine
• Ramipril
• Ranolazine
• Ribociclib
• Ribociclib; Letrozole
• Rifampin
• Ritonavir
• Sapropterin
• Saquinavir
• Sarilumab
• Siltuximab
• Simvastatin
• Simvastatin; Sitagliptin
• Sofosbuvir; Velpatasvir; Voxilaprevir
• St. John’s Wort, Hypericum perforatum
• Sufentanil
• Tamsulosin
• Telithromycin
• Testosterone
• Tezacaftor; Ivacaftor
• Thioridazine
• Tipranavir
• Tocilizumab
• Tofacitinib
• Tramadol
• Trandolapril
• Trandolapril; Verapamil
• Trimipramine
• Tuberculin Purified Protein Derivative, PPD
• Tucatinib
• Ubrogepant
• Upadacitinib
• Venetoclax
• Venlafaxine
• Verapamil
• Vinorelbine
• Voriconazole