Imatinib

Imatinib Brand Name– Gleevec

What is Imatinib

Imatinib is an oral BCR-ABL tyrosine kinase inhibitor.

It is indicated for the treatment of adults and pediatric patients with newly diagnosed chronic-phase Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML); chronic-phase, accelerated-phase, or myeloid or lymphoid blast-phase Ph+ CML after failure of interferon-alfa therapy; relapsed or refractory Ph+ acute lymphoblastic leukemia (ALL); myelodysplastic/myeloproliferative diseases associated with platelet-derived growth factor receptor; aggressive systemic mastocytosis without the D816V c-Kit mutation or with c-Kit mutational status unknown; and hypereosinophilic syndrome and/or chronic eosinophilic leukemia. 

It is also indicated for the treatment of unresectable, recurrent and/or metastatic dermatofibrosarcoma protuberans; Kit (CD117)-positive unresectable and/or metastatic malignant gastrointestinal stromal tumors; and in pediatric patients 1 year of age and older with newly diagnosed Ph+ ALL in combination with chemotherapy.

Severe myelosuppression, congestive heart failure, and hepatotoxicity have been reported.

Indications

1. acute lymphocytic leukemia (ALL)
2. chronic eosinophilic leukemia (CEL)
3. chronic myelogenous leukemia (CML)
4. dermatofibrosarcoma protuberans
5. desmoid tumor
6. gastrointestinal stromal tumors (GIST)
7. hypereosinophilic syndrome
8. myelodysplastic syndrome (MDS)
9. systemic mastocytosis

For the treatment of Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML)

NOTE: The FDA has designated imatinib as an orphan drug for the treatment of CML.

Side Effects

1. abdominal pain
2. abdominal pain
3. acute generalized exanthematous pustulosis (AGEP)
4. alopecia
5. alopecia
6. anaphylactic shock
7. anasarca
8. anemia
9. anemia
10. angina
11. angioedema
12. anorexia
13. anorexia
14. anxiety
15. anxiety
16. aplastic anemia
17. appetite stimulation
18. arrhythmia exacerbation
19. arthralgia
20. arthralgia
21. ascites
22. asthenia
23. asthenia
24. atrial fibrillation
25. avascular necrosis
26. back pain
27. back pain
28. bleeding
29. bleeding
30. blepharitis
31. blurred vision
32. blurred vision
33. bone pain
34. bone pain
35. breast enlargement
36. bullous rash
37. cardiac arrest
38. cardiac tamponade
39. cataracts
40. cerebral edema
41. cheilitis
42. chest pain (unspecified)
43. chest pain (unspecified)
44. chills
45. chills
46. clastogenesis
47. colitis
48. confusion
49. conjunctivitis
50. constipation
51. constipation
52. cough
53. cough
54. dehydration
55. depression
56. depression
57. diarrhea
58. diarrhea
59. dizziness
60. dizziness
61. drowsiness
62. Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)
63. dysgeusia
64. dyspepsia
65. dyspepsia
66. dysphagia
67. dyspnea
68. dyspnea
69. ecchymosis
70. edema
71. edema
72. elevated hepatic enzymes
73. eosinophilia
74. epistaxis
75. eructation
76. erythema
77. erythema multiforme
78. esophagitis
79. exfoliative dermatitis
80. fatigue
81. fatigue
82. fever
83. fever
84. flatulence
85. flatulence
86. fluid retention
87. fluid retention
88. flushing
89. folliculitis
90. gastritis
91. gastroesophageal reflux
92. GI bleeding
93. GI obstruction
94. GI perforation
95. gout
96. growth inhibition
97. gynecomastia
98. headache
99. headache
100. hearing loss
101. heart failure
102. hematemesis
103. hematoma
104. hematuria
105. hemolytic anemia
106. hepatic failure
107. hepatic necrosis
108. hepatitis
109. hyperamylasemia
110. hyperbilirubinemia
111. hyperbilirubinemia
112. hypercalcemia
113. hyperglycemia
114. hyperglycemia
115. hyperhidrosis
116. hyperkalemia
117. hypertension
118. hypertension
119. hyperuricemia
120. hypoalbuminemia
121. hypoalbuminemia
122. hypocalcemia
123. hypocalcemia
124. hypokalemia
125. hypokalemia
126. hypomagnesemia
127. hyponatremia
128. hypophosphatemia
129. hypotension
130. hypothyroidism
131. hypoxia
132. ileus
133. impotence (erectile dysfunction)
134. increased intracranial pressure
135. increased urinary frequency
136. infection
137. infection
138. influenza
139. influenza
140. insomnia
141. insomnia
142. intracranial bleeding
143. jaundice
144. lacrimation
145. lethargy
146. lethargy
147. leukopenia
148. leukopenia
149. libido decrease
150. lichen planus-like eruption
151. lymphadenopathy
152. lymphopenia
153. lymphopenia
154. macular edema
155. malaise
156. malaise
157. melena
158. memory impairment
159. menorrhagia
160. menstrual irregularity
161. migraine
162. muscle cramps
163. muscle cramps
164. musculoskeletal pain
165. musculoskeletal pain
166. myalgia
167. myalgia
168. myocardial infarction
169. myopathy
170. nail discoloration
171. nausea
172. nausea
173. nephrotoxicity
174. neutropenia
175. neutropenia
176. night sweats
177. night sweats
178. ocular hemorrhage
179. ocular irritation
180. ocular pain
181. optic neuritis
182. oral ulceration
183. osteonecrosis
184. palmar-plantar erythrodysesthesia (hand and foot syndrome)
185. palpitations
186. pancreatitis
187. pancytopenia
188. papilledema
189. paresthesias
190. paresthesias
191. peptic ulcer
192. pericardial effusion
193. pericarditis
194. peripheral edema
195. peripheral edema
196. peripheral neuropathy
197. petechiae
198. pharyngitis
199. pharyngitis
200. photosensitivity
201. pleural effusion
202. pneumonitis
203. pruritus
204. pruritus
205. pseudoporphyria
206. psoriasis
207. pulmonary edema
208. pulmonary fibrosis
209. pulmonary hypertension
210. purpura
211. rash
212. rash
213. renal failure (unspecified)
214. restless legs syndrome (RLS)
215. retinal hemorrhage
216. rhabdomyolysis
217. rhinitis
218. sinus tachycardia
219. sinusitis
220. sinusitis
221. skin hyperpigmentation
222. skin hypopigmentation
223. Stevens-Johnson syndrome
224. stomatitis
225. stomatitis
226. subdural hematoma
227. syncope
228. testicular swelling
229. thrombocytopenia
230. thromboembolism
231. thrombosis
232. thrombotic microangiopathy
233. tinnitus
234. toxic epidermal necrolysis
235. tremor
236. tumor lysis syndrome (TLS)
237. urticaria
238. vasculitis
239. vertigo
240. vesicular rash
241. vomiting
242. vomiting
243. weakness
244. weight gain
245. weight gain
246. weight loss
247. xerophthalmia
248. xerosis
249. xerosis
250. xerostomia

Monitoring Parameters

• CBC with differential
• LFTs
• pregnancy testing
• serum creatinine/BUN
• serum electrolytes
• serum uric acid
• weight

Contraindications

• ascites
• bleeding
• bone marrow suppression
• breast-feeding
• cardiac disease
• children
• contraception requirements
• diabetes mellitus
• driving or operating machinery
• edema
• fungal infection
• geriatric
• GI bleeding
• growth inhibition
• heart failure
• hemochromatosis
• hepatic disease
• herpes infection
• hypertension
• immunosuppression
• infants
• infection
• jaundice
• neonates
• nephrotoxicity
• neutropenia
• pericardial effusion
• pleural effusion
• pregnancy
• pregnancy testing
• pulmonary edema
• renal disease
• renal impairment
• reproductive risk
• thrombocytopenia
• vaccination
• varicella
• ventricular dysfunction
• viral infection

Interactions

• Abciximab
• Abemaciclib
• Acalabrutinib
• Acetaminophen
• Acetaminophen; Aspirin, ASA; Caffeine
• Acetaminophen; Butalbital
• Acetaminophen; Butalbital; Caffeine
• Acetaminophen; Butalbital; Caffeine; Codeine
• Acetaminophen; Caffeine
• Acetaminophen; Caffeine; Dihydrocodeine
• Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
• Acetaminophen; Caffeine; Phenyltoloxamine; Salicylamide
• Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
• Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
• Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
• Acetaminophen; Codeine
• Acetaminophen; Dextromethorphan
• Acetaminophen; Dextromethorphan; Doxylamine
• Acetaminophen; Dextromethorphan; Guaifenesin; Phenylephrine
• Acetaminophen; Dextromethorphan; Phenylephrine
• Acetaminophen; Dextromethorphan; Pseudoephedrine
• Acetaminophen; Dichloralphenazone; Isometheptene
• Acetaminophen; Diphenhydramine
• Acetaminophen; Guaifenesin; Phenylephrine
• Acetaminophen; Hydrocodone
• Acetaminophen; Oxycodone
• Acetaminophen; Pentazocine
• Acetaminophen; Propoxyphene
• Acetaminophen; Pseudoephedrine
• Acetaminophen; Tramadol
• Alfentanil
• Alfuzosin
• Aliskiren; Amlodipine
• Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
• Alpha interferons
• Alprazolam
• 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
• Amobarbital
• Amoxapine
• Amoxicillin; Clarithromycin; Lansoprazole
• Amoxicillin; Clarithromycin; Omeprazole
• Anagrelide
• Antithrombin III
• Antithymocyte Globulin
• Apalutamide
• Aprepitant, Fosaprepitant
• Aripiprazole
• Artemether; Lumefantrine
• Artesunate
• Aspirin, ASA; Butalbital; Caffeine
• Aspirin, ASA; Butalbital; Caffeine; Codeine
• Aspirin, ASA; Caffeine; Dihydrocodeine
• Aspirin, ASA; Carisoprodol; Codeine
• Aspirin, ASA; Dipyridamole
• Aspirin, ASA; Oxycodone
• Atazanavir; Cobicistat
• Atomoxetine
• Atorvastatin
• Atorvastatin; Ezetimibe
• Atropine; Hyoscyamine; Phenobarbital; Scopolamine
• Avanafil
• Avapritinib
• Bacillus Calmette-Guerin Vaccine, BCG
• Barbiturates
• Bedaquiline
• Belladonna Alkaloids; Ergotamine; Phenobarbital
• Benzhydrocodone; Acetaminophen
• Bepridil
• Bicalutamide
• Boceprevir
• Bortezomib
• Bosutinib
• Brexpiprazole
• Brigatinib
• Brimonidine; Timolol
• Bromocriptine
• Brompheniramine; Dextromethorphan; Guaifenesin
• Brompheniramine; Dextromethorphan; Phenylephrine
• Brompheniramine; Guaifenesin; Hydrocodone
• Brompheniramine; Hydrocodone; Pseudoephedrine
• Bupivacaine
• Bupivacaine Liposomal
• Bupivacaine; Lidocaine
• Buprenorphine
• Buprenorphine; Naloxone
• Buspirone
• Butabarbital
• Caffeine; Ergotamine
• Cannabidiol
• Carbamazepine
• Carbinoxamine; Dextromethorphan; Pseudoephedrine
• Carbinoxamine; Hydrocodone; Phenylephrine
• Carbinoxamine; Hydrocodone; Pseudoephedrine
• Cariprazine
• Carvedilol
• Ceritinib
• Cevimeline
• Chlordiazepoxide
• Chlordiazepoxide; Clidinium
• Chlorpheniramine; Codeine
• Chlorpheniramine; Dextromethorphan
• Chlorpheniramine; Dextromethorphan; Phenylephrine
• Chlorpheniramine; Dihydrocodeine; Phenylephrine
• Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
• Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
• Chlorpheniramine; Hydrocodone
• Chlorpheniramine; Hydrocodone; Phenylephrine
• Chlorpheniramine; Hydrocodone; Pseudoephedrine
• Cilostazol
• Cimetidine
• Ciprofloxacin
• Cisapride
• Clarithromycin
• Clomipramine
• Clonazepam
• Clorazepate
• Clozapine
• Cobicistat
• Cobimetinib
• Codeine
• Codeine; Guaifenesin
• Codeine; Phenylephrine; Promethazine
• Codeine; Promethazine
• Colchicine
• Colchicine; Probenecid
• Conivaptan
• Conjugated Estrogens
• Conjugated Estrogens; Bazedoxifene
• Conjugated Estrogens; Medroxyprogesterone
• Crizotinib
• Cyclophosphamide
• Cyclosporine
• Dabigatran
• Daclatasvir
• Dalteparin
• Danaparoid
• Dapagliflozin; Saxagliptin
• Dapsone
• Darifenacin
• Darunavir; Cobicistat
• Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
• Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
• Deflazacort
• Delavirdine
• Desipramine
• Desirudin
• Dexamethasone
• Dexchlorpheniramine; Dextromethorphan; Pseudoephedrine
• Dextromethorphan
• Dextromethorphan; Diphenhydramine; Phenylephrine
• Dextromethorphan; Guaifenesin
• Dextromethorphan; Guaifenesin; Phenylephrine
• Dextromethorphan; Guaifenesin; Potassium Guaiacolsulfonate
• Dextromethorphan; Guaifenesin; Pseudoephedrine
• Dextromethorphan; Promethazine
• Dextromethorphan; Quinidine
• Diazepam
• Diclofenac
• Diclofenac; Misoprostol
• Dienogest; Estradiol valerate
• Digoxin
• Dihydrocodeine; Guaifenesin; Pseudoephedrine
• Dihydroergotamine
• Diltiazem
• Diphenhydramine; Hydrocodone; Phenylephrine
• Diphenhydramine; Ibuprofen
• Diphenhydramine; Naproxen
• Dipyridamole
• Disopyramide
• Docetaxel
• Dofetilide
• Dolutegravir; Rilpivirine
• Donepezil
• Donepezil; Memantine
• Dorzolamide; Timolol
• Doxepin
• Doxercalciferol
• Doxorubicin
• Dronabinol
• Drospirenone; Estradiol
• Dutasteride
• Dutasteride; Tamsulosin
• Duvelisib
• Echinacea
• Efavirenz
• Efavirenz; Emtricitabine; Tenofovir
• Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
• Elagolix; Estradiol; Norethindrone acetate
• Elbasvir; Grazoprevir
• Eletriptan
• Elexacaftor; tezacaftor; ivacaftor
• Eliglustat
• Eltrombopag
• Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
• Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
• Emtricitabine; Rilpivirine; Tenofovir alafenamide
• Emtricitabine; Rilpivirine; Tenofovir disoproxil fumarate
• Enalapril; Felodipine
• Encainide
• Encorafenib
• Enoxaparin
• Entrectinib
• Enzalutamide
• Eplerenone
• Eptifibatide
• Ergoloid Mesylates
• Ergonovine
• Ergot alkaloids
• Ergotamine
• Erythromycin
• Erythromycin; Sulfisoxazole
• Esomeprazole; Naproxen
• Estazolam
• Esterified Estrogens
• Esterified Estrogens; Methyltestosterone
• Estradiol
• Estradiol Cypionate; Medroxyprogesterone
• Estradiol; Levonorgestrel
• Estradiol; Norethindrone
• Estradiol; Norgestimate
• Estradiol; Progesterone
• Estropipate
• Eszopiclone
• Ethinyl Estradiol; Etonogestrel
• Etodolac
• Etonogestrel
• Etravirine
• Everolimus
• Ezetimibe; Simvastatin
• Famotidine; Ibuprofen
• Felodipine
• Fenoprofen
• Fentanyl
• Fesoterodine
• Flecainide
• Flibanserin
• Fluconazole
• Fluoxetine
• Fluoxetine; Olanzapine
• Flurazepam
• Flurbiprofen
• Fluvastatin
• Fondaparinux
• food
• Fostamatinib
• Glecaprevir; Pibrentasvir
• Glimepiride
• Glimepiride; Pioglitazone
• Glimepiride; Rosiglitazone
• grapefruit juice
• Guaifenesin; Hydrocodone
• Guaifenesin; Hydrocodone; Pseudoephedrine
• Guanfacine
• Halofantrine
• Haloperidol
• Heparin
• Homatropine; Hydrocodone
• Hydrochlorothiazide, HCTZ; Losartan
• Hydrochlorothiazide, HCTZ; Metoprolol
• Hydrochlorothiazide, HCTZ; Propranolol
• Hydrocodone
• Hydrocodone; Ibuprofen
• Hydrocodone; Phenylephrine
• Hydrocodone; Potassium Guaiacolsulfonate
• Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
• Hydrocodone; Pseudoephedrine
• Ibrutinib
• Ibuprofen
• Ibuprofen; Oxycodone
• Ibuprofen; Pseudoephedrine
• Idelalisib
• Ifosfamide
• Imipramine
• Indomethacin
• Influenza Virus Vaccine
• Interferon Alfa-2a
• Interferon Alfa-2b
• Interferon Alfa-2b; Ribavirin
• Interferon Alfa-n3
• Interferon Alfacon-1
• Intranasal Influenza Vaccine
• Isavuconazonium
• Isoniazid, INH; Pyrazinamide, PZA; Rifampin
• Isoniazid, INH; Rifampin
• Isradipine
• Itraconazole
• Ivabradine
• Ivacaftor
• Ivosidenib
• Ixabepilone
• Ketoconazole
• Ketoprofen
• Ketorolac
• Lansoprazole; Naproxen
• Lefamulin
• Lemborexant
• Lesinurad
• Lesinurad; Allopurinol
• Letermovir
• Levobupivacaine
• Levomethadyl
• Lidocaine
• Lidocaine; Prilocaine
• Live Vaccines
• Lomitapide
• Loperamide
• Loperamide; Simethicone
• Losartan
• Lovastatin
• Lovastatin; Niacin
• Lumacaftor; Ivacaftor
• Lumacaftor; Ivacaftor
• Lumateperone
• Lurasidone
• Lurbinectedin
• Maprotiline
• Maraviroc
• Measles Virus; Mumps Virus; Rubella Virus; Varicella Virus Vaccine, Live
• Measles/Mumps/Rubella Vaccines, MMR
• Meclofenamate Sodium
• Mefenamic Acid
• Mefloquine
• Meloxicam
• Mephobarbital
• Metformin; Repaglinide
• Metformin; Saxagliptin
• Methadone
• Methamphetamine
• Methohexital
• Methylergonovine
• Methysergide
• Metoprolol
• Mexiletine
• Midazolam
• Mifepristone
• Mitotane
• Nabumetone
• Naloxegol
• Nanoparticle Albumin-Bound Paclitaxel
• Naproxen
• Naproxen; Pseudoephedrine
• Naproxen; Sumatriptan
• Nebivolol
• Nebivolol; Valsartan
• Nefazodone
• Neratinib
• Netupitant, Fosnetupitant; Palonosetron
• Nevirapine
• Niacin; Simvastatin
• Nicardipine
• Nifedipine
• Nilotinib
• Nimodipine
• Nisoldipine
• Nortriptyline
• Olaparib
• Ombitasvir; Paritaprevir; Ritonavir
• Omeprazole; Amoxicillin; Rifabutin
• Oritavancin
• Osimertinib
• Oxaprozin
• Oxybutynin
• Oxycodone
• Paclitaxel
• Paricalcitol
• Paroxetine
• Pazopanib
• Peginterferon Alfa-2a
• Peginterferon Alfa-2b
• Pemigatinib
• Pentobarbital
• Pentosan
• Pergolide
• Perindopril; Amlodipine
• Perphenazine
• Perphenazine; Amitriptyline
• Pexidartinib
• Phenobarbital
• Phentermine; Topiramate
• Pimozide
• Piroxicam
• Ponatinib
• Porfimer
• Posaconazole
• Prednisone
• Primidone
• Propafenone
• Propoxyphene
• Propranolol
• Protease inhibitors
• Protriptyline
• Quazepam
• Quetiapine
• Quinidine
• Ramelteon
• Ranolazine
• Repaglinide
• Ribociclib
• Ribociclib; Letrozole
• Rifabutin
• Rifampin
• Rifamycins
• Rifapentine
• Rilpivirine
• Rimegepant
• Rivaroxaban
• Rolapitant
• Romidepsin
• Rotavirus Vaccine
• Rubella Virus Vaccine Live
• Rufinamide
• Ruxolitinib
• Safinamide
• Sapropterin
• Saxagliptin
• Secobarbital
• Segesterone Acetate; Ethinyl Estradiol
• Selpercatinib
• Selumetinib
• Sertraline
• Sibutramine
• Sildenafil
• Silodosin
• Simeprevir
• Simvastatin
• Simvastatin; Sitagliptin
• Siponimod
• Sirolimus
• Smallpox and Monkeypox Vaccine, Live, Nonreplicating
• Smallpox Vaccine, Vaccinia Vaccine
• Sofosbuvir; Velpatasvir
• Sofosbuvir; Velpatasvir; Voxilaprevir
• Sonidegib
• St. John’s Wort, Hypericum perforatum
• Sufentanil
• Sulindac
• Suvorexant
• Tacrolimus
• Tadalafil
• Tafamidis
• Tamsulosin
• Tasimelteon
• Tazemetostat
• Tedizolid
• Telaprevir
• Telithromycin
• Telotristat Ethyl
• Terbinafine
• Tezacaftor; Ivacaftor
• Thiopental
• Thioridazine
• Thyroid hormones
• Ticlopidine
• Timolol
• Tinzaparin
• Tirofiban
• Tolbutamide
• Tolmetin
• Tolterodine
• Tolvaptan
• Topiramate
• Tramadol
• Trandolapril; Verapamil
• Triazolam
• Tricyclic antidepressants
• Trimetrexate
• Trimipramine
• Tucatinib
• Typhoid Vaccine
• Ubrogepant
• Ulipristal
• Vardenafil
• Varicella-Zoster Virus Vaccine, Live
• Vemurafenib
• Venetoclax
• Venlafaxine
• Verapamil
• Verteporfin
• Vinblastine
• Vincristine
• Vincristine Liposomal
• Vinorelbine
• Vorapaxar
• Voriconazole
• Warfarin
• Yellow Fever Vaccine, Live
• Zanubrutinib
• Ziprasidone
• Zolpidem