Disclaimer:
Medidex is not a provider of medical services and all information is provided for the convenience of the user. No medical decisions should be made based on the information provided on this website without first consulting a licensed healthcare provider.This website is intended for persons 18 years or older. No person under 18 should consult this website without the permission of a parent or guardian.
Iclusig
Overview
What is Iclusig?
Iclusig (ponatinib) is a kinase inhibitor. The chemical name for ponatinib hydrochloride is 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide hydrochloride. The molecular formula is CHClFNO which corresponds to a formula weight of 569.02 g/mol. Its structure is shown below:
Ponatinib HCl is an off-white to yellow powder with pKa of 2.77 and 7.8. The solubility of ponatinib in pH 1.7, 2.7, and 7.5 buffers is 7790 mcg/ml, 3.44 mcg/ml, and 0.16 mcg/ml, respectively, indicating a decrease in solubility with increasing pH. Iclusig tablets are available as white, round, film-coated tablets for oral administration. Each tablet contains ponatinib hydrochloride equivalent to 15, 30 or 45 mg ponatinib with the following inactive ingredients: lactose monohydrate, microcrystalline cellulose, sodium starch glycolate (type B), colloidal silicon dioxide, magnesium stearate and a tablet coating. The tablet coating consists of talc, polyethylene glycol, polyvinyl alcohol, and titanium dioxide.
What does Iclusig look like?
What are the available doses of Iclusig?
Tablets: 15 mg, 30 mg and 45 mg ()
What should I talk to my health care provider before I take Iclusig?
How should I use Iclusig?
Iclusig (ponatinib) is a kinase inhibitor indicated for the:
The optimal dose of Iclusig has not been identified. In clinical trials, the starting dose of Iclusig was 45 mg administered orally once daily. However, in the phase 2 trial, 68% of the patients required dose reductions to 30 mg or 15 mg once daily during the course of therapy.
Start dosing with 45 mg once daily. Consider reducing the dose of Iclusig for patients with chronic phase (CP) CML and accelerated phase (AP) CML who have achieved a major cytogenetic response.
Consider discontinuing Iclusig if response has not occurred by 3 months (90 days).
Iclusig may be taken with or without food. Tablets should be swallowed whole.
What interacts with Iclusig?
Sorry No Records found
What are the warnings of Iclusig?
Sorry No Records found
What are the precautions of Iclusig?
Sorry No Records found
What are the side effects of Iclusig?
Sorry No records found
What should I look out for while using Iclusig?
None.
What might happen if I take too much Iclusig?
Overdoses with Iclusig were reported in clinical trials. One patient was accidentally administered the entire contents of a bottle of study medication via nasogastric tube. The investigator estimated that the patient received 540 mg of Iclusig. Two hours after the overdose, the patient had an uncorrected QT interval of 520 ms. Subsequent ECGs showed normal sinus rhythm with uncorrected QT intervals of 480 and 400 ms. The patient died 9 days after the overdose from pneumonia and sepsis. Another patient accidentally self-administered 165 mg on cycle 1 day 2. The patient experienced fatigue and non-cardiac chest pain on day 3. Multiple doses of 90 mg per day for 12 days in a patient resulted in pneumonia, systemic inflammatory response, atrial fibrillation, and a moderate pericardial effusion.
In the event of an overdose of Iclusig, stop Iclusig, observe the patient and provide appropriate supportive treatment.
How should I store and handle Iclusig?
Do not use after the expiration date.Not in-use (unopened) ADMELOG should be stored in a refrigerator (36°F-46°F [2°C-8°C]), but not in the freezer. Do not use ADMELOG if it has been frozen.In-use (opened) ADMELOG vials and ADMELOG SoloStar pens should be stored at room temperature (below 86°F [30°C]) and must be used within 28 days or be discarded, even if they still contain ADMELOG. Protect from direct heat and light.See :Do not use after the expiration date.Not in-use (unopened) ADMELOG should be stored in a refrigerator (36°F-46°F [2°C-8°C]), but not in the freezer. Do not use ADMELOG if it has been frozen.In-use (opened) ADMELOG vials and ADMELOG SoloStar pens should be stored at room temperature (below 86°F [30°C]) and must be used within 28 days or be discarded, even if they still contain ADMELOG. Protect from direct heat and light.See :Do not use after the expiration date.Not in-use (unopened) ADMELOG should be stored in a refrigerator (36°F-46°F [2°C-8°C]), but not in the freezer. Do not use ADMELOG if it has been frozen.In-use (opened) ADMELOG vials and ADMELOG SoloStar pens should be stored at room temperature (below 86°F [30°C]) and must be used within 28 days or be discarded, even if they still contain ADMELOG. Protect from direct heat and light.See :Do not use after the expiration date.Not in-use (unopened) ADMELOG should be stored in a refrigerator (36°F-46°F [2°C-8°C]), but not in the freezer. Do not use ADMELOG if it has been frozen.In-use (opened) ADMELOG vials and ADMELOG SoloStar pens should be stored at room temperature (below 86°F [30°C]) and must be used within 28 days or be discarded, even if they still contain ADMELOG. Protect from direct heat and light.See :Iclusig tablets are available in the following configurations.
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
Ponatinib is a kinase inhibitor. Ponatinib inhibited the tyrosine kinase activity of ABL and T315I mutant ABL with IC concentrations of 0.4 and 2.0 nM, respectively. Ponatinib inhibited the activity of additional kinases with IC concentrations between 0.1 and 20 nM, including members of the VEGFR, PDGFR, FGFR, EPH receptors and SRC families of kinases, and KIT, RET, TIE2, and FLT3. Ponatinib inhibited the viability of cells expressing native or mutant BCR-ABL, including T315I. In mice, treatment with ponatinib reduced the size of tumors expressing native or T315I mutant BCR-ABL when compared to controls.
Non-Clinical Toxicology
None.Arterial occlusions, including fatal myocardial infarction, stroke, stenosis of large arterial vessels of the brain, severe peripheral vascular disease have occurred in at least 35% of Iclusig-treated patients from the phase 1 and phase 2 trials. With a minimum of 48 months follow-up for ongoing patients (N=133) in the phase 2 trial, 33% (150/449) of Iclusig-treated patients experienced a cardiac vascular (21%), peripheral vascular (12%), or cerebrovascular (9%) arterial occlusive event; some patients experienced more than 1 type of arterial occlusive event.
Iclusig can cause fatal and life-threatening arterial occlusion within 2 weeks of starting treatment, and at dose levels as low as 15 mg per day. Iclusig can also cause recurrent or multi-site vascular occlusion. Patients have required revascularization procedures (coronary, cerebrovascular, and peripheral arterial).
In the phase 2 trial, the median time to onset of the first cardiac vascular, cerebrovascular, and peripheral vascular arterial occlusive events was 193 (range: 1 - 1355), 526 (range: 5 - 1339), and 478 (range: 3 - 1344) days, respectively.
Patients with and without cardiovascular risk factors, including patients age 50 years or younger, experienced these events. The most common risk factors observed in patients with arterial occlusive events were hypertension (62%; 93/150), hyperlipidemia (61%; 91/150), and history of cardiac disease (48%; 72/150). Arterial occlusion adverse events were more frequent with increasing age and in patients with history of ischemia, hypertension, diabetes, or hyperlipidemia ].
Cardiac vascular occlusion, including fatal and life-threatening myocardial infarction and coronary artery occlusion has occurred in 21% (94/449) of Iclusig-treated patients. Patients have developed heart failure concurrent or subsequent to the myocardial ischemic event
Cerebrovascular occlusion, including fatal stroke, has occurred in 9% (40/449) of Iclusig-treated patients. Iclusig can cause stenosis over multiple segments in major arterial vessels that supply the brain (e.g., carotid, vertebral, middle cerebral artery).
Peripheral arterial occlusion, including fatal mesenteric artery occlusion and life-threatening peripheral arterial disease, have occurred in 12% (52/449) of Iclusig-treated patients. Patients have developed digital or distal extremity necrosis and have required amputations. Renal artery stenosis, associated with worsening, labile or treatment-resistant hypertension, has occurred in some Iclusig-treated patients .
Clinicians should consider whether the benefits of Iclusig treatment are expected to exceed the risks of therapy. In patients suspected of developing arterial occlusive events, interrupt or stop Iclusig. A benefit-risk consideration should guide a decision to restart Iclusig therapy .
The following adverse reactions are discussed in greater detail in other sections of the prescribing information:
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
While we update our database periodically, we cannot guarantee it is always updated to the latest version.
Review
Read user comments about the side effects, benefits, and effectiveness of losartan oral.
Overall User Ratings
517Total User Reviews
User Reviews
Learn about
User Reviews
Professional
Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72Tips
Tips
Interactions
Interactions
A total of 440 drugs (1549 brand and generic names) are known to interact with Imbruvica (ibrutinib). 228 major drug interactions (854 brand and generic names) 210 moderate drug interactions (691 brand and generic names) 2 minor drug interactions (4 brand and generic names) Show all medications in the database that may interact with Imbruvica (ibrutinib).