1 / 75

New Drug Update 2012

New Drug Update 2012. Nancy Letassy, PharmD, CDE Professor University of Oklahoma College of Pharmacy. 2012. New Molecular entities. Belviq ® (locaserin).

Download Presentation

New Drug Update 2012

An Image/Link below is provided (as is) to download presentation Download Policy: Content on the Website is provided to you AS IS for your information and personal use and may not be sold / licensed / shared on other websites without getting consent from its author. Content is provided to you AS IS for your information and personal use only. Download presentation by click this link. While downloading, if for some reason you are not able to download a presentation, the publisher may have deleted the file from their server. During download, if you can't get a presentation, the file might be deleted by the publisher.


Presentation Transcript

  1. New Drug Update 2012 Nancy Letassy, PharmD, CDE Professor University of Oklahoma College of Pharmacy

  2. 2012 NewMolecularentities

  3. Belviq® (locaserin) • Approved as an adjunct to a reduced caloric diet and increased activity for chronic weight management in adult with a BMI of >30 or >27 in presence of type 2 diabetes, hypertension, or dyslipidemia • Serotonin 2c agonist that activates receptor in the brain to decrease food consumption and promote satiety.

  4. Belviq® (locaserin) Adverse reactions: • Headache, dizziness, euphoria, cognitive impairment, hallucinations • Fatigue, dry mouth, diarrhea, constipation • Hypoglycemia in patients on a glucose lowering agent • Bradycardia • Decreased white and red blood cells

  5. Qsymia® (phentermine and topiramate) • Indicated for chronic weight management in obese or overweight adults with at least one weight-related comorbidity such as hypertension, type 2 diabetes or dyslipidemia • Combines low doses of phentermine and extended-release topiramate • Weight loss on average 20 pounds in one year • Previously called Qnexa®

  6. Qsymia® ADR • cognition, fatigue, dizziness, dysgeusia, insomnia, constipation, dry mouth, tachycardia, depression, anxiety, kidney stones, decreased sweating and increased body temperature, hypokalemia, metabolic acidosis, hypoglycemia, hypotension.

  7. Qsymia® • Ensure adequate fluid intake to decrease risk of renal stones • Advise patients to watch for decreased sweating and increased body temperature with increased physical activity in hot weather

  8. Qsymia®ADR • Monitor for suicidal thoughts and behavior • Monthly pregnancy tests • Monitor blood pressure • Monitor blood glucose in those on glucose lowering agents • Check potassium, bicarbonate, creatinine, and other electrolytes

  9. Elelyso® (taliglucerase alfa) • Hydrolytic, lysosomal, glucocerebroside-specific enzyme indicated for a long-term enzyme replacement therapy (ERT) for adults with a confirmed diagnosis of Type 1 Gaucher disease.

  10. Gaucher Disease • Most common form: Type 1 non-neurological • Cause: absence of glucocerebrosidase in lysosomes • Fatty material accumulates in spleen and liver • Symptoms can begin early in life or adulthood • Spleen, liver, lungs, brain and bone marrow affected • Increased bruising, fatigue, increased fractures, lung and kidney impairment, anemia • Autosomal recessive

  11. Treatment of Gaucher Disease • Current treatment • Enzyme replacement therapy (ERT) • Cerezyme®: mammalian cell –recombinant • 10-15% antibodies; allergic reactions • VPRIV®: human cell recombinant • Elelyso®: plant cell recombinant

  12. Eleyso® • Gene for human enzyme is inserted into carrot cells. • Decreases liver and spleen volume, anemia, increases platelets. • Dose: 60 units/kg IV over 1-2 hours every 2 weeks • Adverse Drug Reactions • Infusion reactions--Usually mild • Reduce risk by slow infusion rate, pretreat with antihistamines or corticosteroids • Common ADRs • URI, throat infections, UTI, extremity pain

  13. Chemotherapeutic agents

  14. Erivedge® (vismodegib) • First and only oral agent approved for treatment of adults with metastatic basal cell cancer (BCC) or locally advanced BCC recurrent post-surgery or those not candidates for surgery or radiation

  15. Erivedge® MOA • Designed to inhibit selectively the Hedgehog pathway • This pathway is active in the proper development of embryos. • In adults it is less active except for tissue repair and maintenance • . When it malfunctions it can result is diseases like BCC.

  16. Erivedge® Dosing • Dose: 150 mg capsule every day until disease progression or until unacceptable adverse reaction. • Verify pregnancy 7 days before administration. • Embryo-fetal death or severe birth defects can occur • Continue birth control 7 months past last dose. Males using Erivedge encouraged to use a condom with spermicide even if post-vasectomy while on medication and two months thereafter. • Do not donate blood or blood products while taking this drug and for 7 months after last dose.

  17. Erivedge® ADRs • GI: change in how things taste or loss of taste, nausea, diarrhea, decreased appetite, constipation and vomiting • Joint aches, Muscle spasms • Hair loss • Weight loss • Tiredness

  18. Inlyta® (axitinib) • Kinase inhibitor for the treatment of advanced renal cell carcinoma (RCC) after failure of one prior systemic therapy. • Inhibits vascular endothelial growth factor receptors (VEGFR)-1, VEGFR-2, and VEGFR-3 • These receptors are implicated in pathologic angiogenesis, tumor growth, and cancer progression.

  19. Inlyta® (axitinib) • 5 to 10 mg PO every 12 hours with a full glass of water. • Reduce dose if liver impairment present or is used with a strong CYP 3A4/5 inhibitor • Avoid grapefruit juice • Both partners need to use effective birth control methods. • Use during pregnancy can cause fetal harm. Most common ADRs (>20%) • GI: diarrhea, decrease in appetite or ability to taste things, weight loss, nausea, vomiting, constipation, stomach pain, heart burn • redness, pain, swelling, numbness, tingling, or itching or peeling of the skin on your hands and feet • Hypertension, dysphonia

  20. Inlyta®Warning and Precautions • The following adverse events have occurred: • Hypertension and hypertensive crises • Arterial and venous thrombotic events fatal and nonfatal • Cerebral and GI bleeding, fatal and nonfatal • Hypothyroidism, proteinuria, increased liver enzymes • Fetal harm

  21. Kyprolis® (carflizomib) • A proteasome inhibitor for advanced multiple myeloma who have not responded to at least two other drugs. • Multiple myeloma is a malignant increase in plasma cells • Multiple myeloma associated with an increase in proteasome levels • Proteasomes present in all cells to degrade unneeded or damaged proteins

  22. Kyprolis® Dosing • Administered IV on two consecutive days every week for 3 weeks followed by a 12 day rest. • Dose: 20-27 mg/m2/day • Common side effects (>30%): nausea, diarrhea, pyrexia, anemia, thrombocytopenia, dyspnea and fatigue

  23. Kyprolis®Warnings and Precautions • Heart failure and ischemia • Pulmonary complications and hypertension • Liver toxicity and failure • Tumor lysis syndrome • Infusion reactions • Fetal harm

  24. Perjeta® (pertuzumab) • Approved for use in combination with Herceptin® and docetaxal for HER2 positive metastatic breast cancer who have not received prior anti-HER2 or chemotherapy for metastatic disease. • HER2 overexpression correlates with aggressive form of breast cancer—25% of all breast tumor • Dysregulation of HER-mediated signaling pathways results in growth and spread of cancer cells • Inappropriate signaling may lead to uncontrolled cell proliferation, decreased cell death, angiogenesis and increased cancer cell motility.

  25. Perjeta® (pertuzumab) • Dose: initial 840 mg IV followed by 420 mg IV every 3 weeks. • Clinical effect: increases progression free survival by 6.1 months

  26. Perjeta® Serious ADR • Fetal death and Birth Defects: birth control during treatment and for 6 months after a patient's last dose of Perjeta. Heart problems: reduced heart function and CHF • Infusion-related reactions: fatigue, loss of taste, allergic reactions, muscle pain, and vomiting • Severe allergic reactions: may be severe, may happen quickly, and may affect many areas of the body

  27. Xtandi ® (enzalutamide) • An androgen receptor inhibitor for treatment of metastatic castration-resistant prostate cancer previously treated with docetaxel • Dose : 160 mg daily

  28. Drug Interactions Avoid co-administration with: • strong CYP2C8 inhibitors (gemfibrozil) and moderate to strong CYP 2C8 inducers (rifampin) • 3A4 inducers (carbamazepine, phenytoin, phenobarbital) or inhibitors (itraconazole), and • Xtandi® is a moderate to strong inducer of 3A4 (cyclosporine), 2C9 (warfarin), 2C19 (omeprazole). This interaction can decrease the effectiveness of these agents.

  29. Zaltrap® (ziv-aflibercept) • Indicated for use in a multiple drug combination in the treatment of metastatic colorectal cancer resistant to or has progressed following an oxaliplatin-containing regimen

  30. Zaltrap®MAO • An angiogenesis inhibitor that results in decreased neovascularization and decreased vascular permeability

  31. Zaltrap® Dosing and ADRs • Dose: 4 mg IV over one hour every two weeks. • Administration continues until disease progression or unacceptable toxicity • Serious adverse reactions: • Hemorrhage • GI perforation • Compromised wound healing • Fistula formation • Hypertension • Arterial thromboembolic events • Proteinuria • Neutropenia

  32. Stivarga® (regorafenib) • Recently approved for the treatment of metastatic colorectal cancer. • Oral novel multikinase inhibitor that blocks multiple enzymes that promote cancer growth • 29% increase in survival versus placebo • Black box warning—severe and fatal liver toxicity occurred during treatment

  33. Bosulif® (bosutinib) • A kinase inhibitor for treatment of chronic myelogenous leukemia (CML) in adults with chronic, accelerated, or blast phase with resistance or intolerance to prior therapy. • CML due to chromosomal abnormality resulting in the formation of Philadelphia chromosome • Abnormal fusion of Brc-Abl tyrosine kinase implicated in pathogenesis of CML • One source of treatment resistance is activation of Src-family kinases.

  34. Bosulif® (bosutinib) • Dose: 500 – 600 mg daily • Avoid use with strong CYP3A inducers or inhibitors • Avoid use with proton pump inhibitors – decrease drug levels • Common ADR (>20%) • Diarrhea, nausea, thrombocytopenia, • Serious ADR • GI toxicity, Hepatic toxicity, fetal toxicity • Fluid retention • Myelosuppression

  35. FluMist Quadrivalent ® (influenza vaccine live) • Intranasal influenza vaccine containing four strains of the influenza virus. • Indicated for active immunization for the prevention of disease caused by influenza A subtype and B viruses • Approved for use in person 2 through 49 years of age • Administered intranasally—one-half the dose in each nostril

  36. FluMist® Quadrivalent • Do not administer to persons who have had a server allergic reaction to any component: egg protein, gentamicin, gelatin and arginine • Do not administer to children and adolescents through 17 who are on aspirin containing therapy because of risk of Reye’s syndrome Package insert 2012

  37. Menhibrix® • A vaccine for prevention of Neisseria meningitidis (C and Y) and Haemophilus influenzae type b infections in children. • Four doses IM at 2, 4, 6, and 12-15 months.

  38. Kalydeco® (ivacaftor) • Approved for treatment of cystic fibrosis (CF) in patients ≥6 years who have a G551D mutation in the CFTR gene. • Transmembrane conductance regulator (CFTR) potentiator for cystic fibrosis patients with certain gene mutation • Treats the underlying mutation not just the symptoms • CFTR functions as an anion channel. • Found in epithelial cells of the lungs, liver, pancreas, GIT, skin, reproductive tract. • In CF, CFTR defects results in reduced transport of NaCl resulting in build up of sticky mucus

  39. Kalydeco® (ivacaftor) • 150 mg tablet every 12 hours with a high fat meal • Promotes weight gain and improved lung function • Costs $294,000/year. Available for only through specialty pharmacies Adverse Drug Effects • Headache, URI, nasal congestion, nasopharyngitis • Nausea, diarrhea • Rash, dizziness, abdominal pain

  40. Kalydeco® Drug Interactions • Strong 3A4 inhibitors like ketoconazole increases levels 8.5-fold; fluconazole 3-fold • Other drugs like rifampin and St. John’s Wort should be avoided • Kalydeco® has potential to inhibit 3A4, P-glycoprotein, and 2C9. • Check levels of cyclosporine, tacrolimusand digoxin and monitor INR (warfarin)

  41. Myrbetriq® (mirabegron) • Beta-3 adrenergic agonist for overactive bladder • Simulation promotes relaxation of detrusor muscle in the bladder adding in urination

  42. Myrbetriq®(mirabegron) • Dosing: 25 to 50 mg QD • Reduce dose in moderate renal impairment • Warnings and Precautions • Hypertension • Bladder outlet obstruction • Concomitant medications metabolized by CYP2D6. Myrbetriq® is an inhibitor of this pathway. (digoxin)

  43. Omontys® (peginesatide) • Erythropoiesis-stimulating agent (ESA) for anemia in dialysis patients • Not indicated for patients: • with CKD not on dialysis • as a substitute for transfusions in acute situations, • On chemotherapy and have anemia not due to CKD • Without demonstrated benefit • Initial dosing: 0.04 mg/kg/month (injectable) • Dose conversion from another ESA based on total weekly dose at that time.

  44. Omontys® (peginesatide) • Contraindicated in uncontrolled hypertension • Most common ADRs (>10%): dyspnea, diarrhea, cough, nausea, A-V fistula site complications • Warning: Increased risk of MI, stroke and thromboembolism when Hgb increased to >11 gm/dl Package insert

  45. Picato® Gel (ingenol mebutate) • Inducer of cell death indicated in the topical treatment of actinic keratosis • Two strengths: 0.015% and 0.05% gel • Lower strength applied to AK on face and scalp daily for 3 consecutive days • Higher strength applied to AK on trunk and extremities daily for 2 consecutive days

  46. Picato® Gel (ingenol mebutate) Warnings and ADRs • Eye disorders: severe eye pain, ptosis, and edema. • Local skin reactions • : vesiculation, pustulation, pruritis, erosions, ulcerations, infection • Headache, nasopharyngitis

  47. Stendra® (avanafil) • PDE5 inhibitor for erectile dysfunction • Dose 50 to 200 mg 30 minutes prior to sexual activity PRN (no more than one dose in 24 hours) • Do not use with strong CYP3A4 inhibitors • Decrease dose to 50 mg in 24 hours when using a moderate CYP3A4 inhibitor • Lower dose to 50 mg/day in patients on stable alpha-blocker therapy

  48. Stendra® (avanafil) Strong CYP 3A4 inhibitors Moderate CYP 3A4 inhibitors Verapamil Diltiazem Erythromycin Fluconazole Grapefruit juice Ciprofloxacin • Protease inhibitors—ritinovir • Macrolide antibiotics—clarithromycin • Nefazodone • Azole antifungals --ketoconazole

  49. Alpha blockers • Selective α1-adrenergic blockers include: • alfuzoxin (Uroxatral) • prazosin (Minipres) • doxazosin (Cardura) • tamsulosin (Flomax) • terazosin (Hytrin) • silodosin (Rapaflo)

More Related