Abiraterone acetate: It is converted in vivo to abiraterone, an androgen biosynthesis inhibitor, that inhibits 17 a-hydroxylase/C17,20-lyase (CYP17). This enzyme is expressed in testicular, adrenal, and prostatic tumor tissues and is required for androgen biosynthesis. Abiraterone acetate is specifically indicated in combination with prednisone for the treatment of patients with metastatic castration-resistant prostate cancer who have received prior chemotherapy containing docetaxel.
Aflibercept: It is a recombinant fusion protein consisting of portions of human VEGF receptors 1 and 2 extracellular domains fused to the Fc portion of human IgG1 formulated as an iso-osmotic solution for intravitreal administration. Vascular endothelial growth factor-A (VEGF-A) is a member of the VEGF family of angiogenic factors that can act as mitogenic, chemotactic, and vascular permeability factors for endothelial cells. VEGF acts via two receptor tyrosine kinases, VEGFR-1 and VEGFR-2, present on the surface of endothelial cells. Activation of these receptors by VEGF-A can result in neovascularization and vascular permeability. Aflibercept is specifically approved for neovascular (wet) age-related macular degeneration.
Axitinib: It inhibits receptor tyrosine kinases including vascular endothelial growth factor receptors (VEGFR)-1, VEGFR-2, and VEGFR-3. It is specifically approved for the oral treatment of advanced renal cell carcinoma after failure of one prior systemic therapy.
Azilsartan: New angiotensin receptor blocker approved for hypertension.
Belatacept: It is a a selective T-cell (lymphocyte) costimulation blocker. It binds to CD80 and CD86 on antigen-presenting cells, thereby blocking CD28 mediated costimulation of T lymphocytes. It is specifically indicated for the prophylaxis of organ rejection in adult patients receiving a kidney transplant. It is approved for use in combination with basiliximab induction, mycophenolate mofetil, and corticosteroids.
Belimumab: It is a human IgG1 monoclonal antibody specific for soluble human B lymphocyte stimulator protein (BLyS). It blocks the binding of soluble BLyS, a B-cell survival factor, to its receptors on B cells. Belimumab does not bind B cells directly, but by binding BLyS, it inhibits the survival of B cells, including auto reactive B cells, and reduces the differentiation of B cells into immunoglobulin-producing plasma cells. Elevated levels of BLyS are seen in the blood or joint fluid of patients with autoimmune and inflammatory disorders. Belimumab is specifically indicated for the treatment of adult patients with active, autoantibody-positive, systemic lupus erythematosus who are receiving standard therapy. It is given intravenously.
Brentuximab vedotin: It is a CD30-directed antibody-drug conjugate (ADC) consisting of three components: 1) the chimeric IgG1 antibody cAC10, specific for human CD30, 2) the microtubule disrupting agent monomethyl auristatin E (MMAE) and 3) a protease-cleavable linker that covalently attaches MMAE to cAC10. Brentuximab vedotin is designed to be stable in the bloodstream, but to release MMAE upon internalization into CD30-expressing tumor cells, resulting in a targeted cell-killing effect. It is specifically approved for 1) Hodgkin lymphoma after failure of autologous stem cell transplant (ASCT) or after failure of at least two prior multi-agent chemotherapy regimens in patients who are not ASCT candidates and 2) systemic anaplastic large cell lymphoma after failure of at least one prior multi-agent chemotherapy regimen. It is administered intravenously.
Crizotinib: It is an oral selective, ATP-competitive small molecule dual inhibitor of mesenchymal epithelial transition growth factor (c-Met or hepatocyte growth factor) and ALK tyrosine kinases. Crizotinib is specifically approved for the treatment of locally advanced or metastatic non-small cell lung cancer that is anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test.
Eculizumab: It is a monoclonal antibody that specifically binds to the complement protein C5 with high affinity, thereby inhibiting its cleavage to C5a and C5b and preventing the generation of the terminal complement complex C5b-9. It has now been approved for atypical hemolytic uremic syndrome (aHUS) to inhibit complement-mediated thrombotic microangiopathy. It is already being used for paroxysmal nocturnal hemoglobinuria.
Everolimus: It is an inhibitor of mammalian target of rapamycin (mTOR). The mTOR pathway is dysregulated in several human cancers. Everolimus is specifically approved for the treatment of progressive neuroendocrine tumors of pancreatic origin in patients with unresectable, locally advanced or metastatic disease. Everolimus is supplied as a tablet for oral administration.
Ezogabine: It enhances transmembrane potassium currents mediated by the KCNQ family of ion channels. By this mechanism, it is thought to stabilize the resting membrane potential and reduce brain excitability. It is specifically indicated as adjunctive treatment of partial-onset seizures in adults.
Fidaxomicin: It is a narrow-spectrum macrocyclic antibiotic and is bactericidal against C. difficile in vitro. It acts by inhibiting RNA synthesis by RNA polymerases. It is specifically indicated in adults for oral treatment of Clostridium difficile-associated diarrhea. It can cause gastrointestinal hemorrhage, anemia and neutropenia.
Glucarpidase: It contains a recombinant enzyme which rapidly lowers blood levels of methotrexate, reducing its concentration to below the threshold for serious toxicity. It converts methotrexate to its inactive metabolites DAMPA and glutamate. DAMPA and glutamate are metabolized by the liver, providing an alternative route of methotrexate elimination to renal clearance during high-dose methotrexate treatment. It is specifically indicated for the treatment of toxic plasma methotrexate concentrations (>1 micromole per liter) in patients with delayed methotrexate clearance due to impaired renal function. It is administered by i.v. route.
Icatibant: It is a competitive antagonist selective for the bradykinin B2 receptor. Hereditary angioedema (HAE) is caused by an absence or dysfunction of C1-esterase-inhibitor, a key regulator of the Factor XII/kallikrein proteolytic cascade that leads to bradykinin production. Bradykinin is a vasodilator which is thought to be responsible for the characteristic HAE symptoms of localized swelling, inflammation, and pain. Icatibant (given subcutaneously) inhibits bradykinin from binding the B2 receptor and thereby treats the clinical symptoms of an acute, episodic attack of hereditary angioedema. Icatibant is specifically approved for the treatment of acute attacks of hereditary angioedema in adults.
Indacaterol: It is a long-acting β2-adrenergic agonist like salmeterol and formoterol. It is specifically approved for the treatment of airflow obstruction in patients with chronic obstructive pulmonary disease, including chronic bronchitis and/or emphysema.
Ingenol mebutate: It is an inducer of apoptosis and is indicated for the topical treatment of actinic keratosis of the face, scalp, trunk and extremities.
Ipilimumab: It is a recombinant, human monoclonal antibody that binds to the cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4), a molecule on T cells that suppresses the immune response. CTLA-4 is a negative regulator of T-cell activation. Ipilimumab binds to CTLA-4 and blocks the interaction of CTLA-4 with its ligands. Blockade of CTLA-4 has been shown to augment T-cell activation and proliferation. The mechanism of action of ipilimumab’s effect in patients with melanoma is indirect, possibly through T-cell mediated anti-tumor immune responses. It is specifically indicated for the treatment of unresectable or metastatic melanoma. It is i administered by intravenous route.
Ivacaftor: It is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator. Cystic fibrosis is caused by mutations in a gene that encodes for the CFTR protein that regulates ion (such as chloride) and water transport in the body. The defect in chloride and water transport results in the formation of thick mucus that builds up in the lungs, digestive tract and other parts of the body leading to severe respiratory and digestive problems. It was specifically approved for the treatment of cystic fibrosis in patients age 6 years and older who have a G551D mutation in the CFTR gene. It is given orally for this indication.
Linagliptin: It is a newer orally-active inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme similar to sitagliptin and is approved for type 2 diabetes mellitus. Major adverse effect of this drug include nasopharyngitis, hypoglycemia and pancreatitis
Mifepristone: A small-molecule progesterone and glucocorticoid antagonist has now been approved to control hyperglycemia secondary to hypercortisolism in adults with endogenous Cushing's syndrome who have type II diabetes mellitus or glucose intolerance and have failed surgery or are not candidates for surgery
Rilpivirine: A newer non-nucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus type 1 (HIV-1) similar to etravirine.
Rivaroxaban: It selective oral blocker of the active site of factor Xa and does not require a cofactor (such as Anti-thrombin III) for activity. It is indicated for the prophylaxis of deep vein thrombosis, which may lead to pulmonary embolism in patients undergoing knee or hip replacement surgery.
Ruxolitinib: It inhibits Janus associated kinases; JAK1 and JAK2, which mediate the signaling of a number of cytokines and growth factors that are important for hematopoiesis and immune function. JAK signaling involves recruitment of STATs (signal transducers and activators of transcription) to cytokine receptors, activation and subsequent localization of STATs to the nucleus leading to modulation of gene expression. Myelofibrosis is a myeloproliferative neoplasm known to be associated with dysregulated JAK1 and JAK2 signaling. Ruxolitinib is approved for oral treatment of intermediate or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia vera myelofibrosis and post-essential thrombocythemia myelofibrosis. Anemia and thrombocytopenia are adverse effects.
Sunitinib: It is an oral multi-kinase inhibitor and works by blocking multiple molecular targets like vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR), KIT, FLT3 and RET etc. It has now been approved for the treatment of progressive, well-differentiated pancreatic neuroendocrine tumors in patients with unresectable locally advanced or metastatic disease. It is being used already for renal cell carcinoma.
Tafluprost: A fluorinated analog of PGF2α like Latanoprost approved for reducing elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension by increasing uveoscleral outflow. It is supplied as ophthalmic solution for local use.
Telaprevir and Boceprevir: These inhibit the hepatitis C protease NS3-4A, an enzyme that is essential for HCV viral replication. Combination of peginterferon alfa and ribavirin with telaprevir or boceprevir is indicated for the treatment of genotype 1 chronic HCV in adults with compensated liver disease, including cirrhosis. These are supplied as tablets for oral administration.
Ticagrelor: It is a reversible oral ADP receptor (P2Y12) antagonist (unlike clopidogrel and ticlopidine which are irreversible antagonists at this receptor). It is indicated to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndrome.
Tocilizumab: It is a recombinant humanized monoclonal antibody against IL-6 receptors. IL-6 is a pleiotropic pro-inflammatory cytokine produced by a variety of cell types including T- and B-cells, lymphocytes, monocytes and fibroblasts. IL-6 is also produced by synovial and endothelial cells leading to local production of IL-6 in joints affected by inflammatory processes such as rheumatoid arthritis. Tocilizumab is specifically indicated for the treatment of active systemic juvenile idiopathic arthritis in patients two years of age and older
Vandetanib: An orally available receptor tyrosine kinase (RTK) inhibitor, which blocks both the vascular endothelial growth factor (VEGF) and the Epidermal Growth Factor (EGF) receptor tyrosine kinase. Blockade of the VEGF receptors limits the growth of new blood vessels, which are vital to supporting the growth of tumors. Without sufficient blood supply, tumor cells become starved for nutrients, slowing or halting growth. Vandetanib is specifically indicated for the treatment of symptomatic or progressive medullary thyroid cancer in patients with unresectable locally advanced or metastatic disease.
Vemurafenib: It is a low molecular weight, orally available, inhibitor of mutated BRAF serine-threonine kinase. It is a selective inhibitor of the activated BRAFV600E gene, a gene found in 70% of malignant melanomas and a significant percentage of other cancers. It is indicated for the treatment of unresectable or metastatic melanoma with BRAFV600E mutation
Vilazodone hydrochloride: It is a selective serotonin reuptake inhibitor and a 5HT1A receptor partial agonist indicated for the treatment of major depressive disorder.
Vismodegib: It is an inhibitor of the hedgehog (Hh) signaling pathway. This pathway is typically over-activated in basal cell carcinoma. It is approved for the treatment of adults with metastatic basal cell carcinoma, or with locally advanced basal cell carcinoma that has recurred following surgery or who are not candidates for surgery, and who are not candidates for radiation
Ticagrelor: It is a reversibly binding oral adenosine diphosphate (ADP) receptor antagonist. It selectively inhibits P2Y12, a key target receptor for ADP. ADP receptor blockade inhibits the action of platelets in the blood, reducing recurrent thrombotic events. Ticagrelor is specifically indicated to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndrome (unstable angina, non-ST elevation myocardial infarction, or ST elevation myocardial infarction). Ticagrelor is supplied as a tablet for oral administration. The recommended initial dose is 180 mg (two 90 mg tablets) loading dose and continue treatment with 90 mg twice daily. After the initial loading dose of aspirin (usually 325 mg), use Ticagrelor with a daily maintenance dose of aspirin of 75-100 mg.
Azilsartan: New angiotensin receptor blocker approved for hypertension
Rivaroxaban: It is a factor Xa inhibitor that selectively blocks the active site of factor Xa and does not require a cofactor (such as Anti-thrombin III) for activity. Activation of factor X to factor Xa (FXa) via the intrinsic and extrinsic pathways plays a central role in the cascade of blood coagulation. Rivaroxaban is specifically indicated for the prophylaxis of deep vein thrombosis, which may lead to pulmonary embolism in patients undergoing knee or hip replacement surgery.
Rivaroxaban is supplied as a tablet for oral administration. The recommended initial dose is 10 mg taken orally once daily with or without food. The initial dose should be taken at least 6 to 10 hours after surgery once hemostasis has been established. For hip replacement surgery a treatment duration of 35 days is recommended. For knee replacement surgery a treatment duration of 12 days is recommended
Icatibant: It is a competitive antagonist selective for the bradykinin B2 receptor. Hereditary angioedema (HAE) is caused by an absence or dysfunction of C1-esterase-inhibitor, a key regulator of the Factor XII/kallikrein proteolytic cascade that leads to bradykinin production. Bradykinin is a vasodilator which is thought to be responsible for the characteristic HAE symptoms of localized swelling, inflammation, and pain. Icatibant inhibits bradykinin from binding the B2 receptor and thereby treats the clinical symptoms of an acute, episodic attack of hereditary angioedema. Icatibant is specifically approved for the treatment of acute attacks of hereditary angioedema in adults. Icatibant is supplied as a solution for subcutaneous administration. The recommended dose is 30 mg administered by subcutaneous injection in the abdominal area. Additional doses may be administered at intervals of at least six hours if response is inadequate or if symptoms recur. No more than three doses may be administered in any 24 hour period
Ipilimumab: It is a recombinant, human monoclonal antibody that binds to the cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4), a molecule on T cells that suppresses the immune response. CTLA-4 is a negative regulator of T-cell activation. Ipilimumab binds to CTLA-4 and blocks the interaction of CTLA-4 with its ligands. Blockade of CTLA-4 has been shown to augment T-cell activation and proliferation. The mechanism of action of ipilimumab’s effect in patients with melanoma is indirect, possibly through T-cell mediated anti-tumor immune responses. It is specifically indicated for the treatment of unresectable or metastatic melanoma. It is supplied as a solution for intravenous administration. The recommended dose of this drug is 3 mg/kg administered intravenously over 90 minutes every three weeks for a total of four doses.
Vemurafenib: It is a low molecular weight, orally available, inhibitor of some mutated forms of BRAF serine-threonine kinase, including BRAFV600E. Vemurafenib also inhibits other kinases in vitro such as CRAF, ARAF, wild-type BRAF, SRMS, ACK1, MAP4K5 and FGR at similar concentrations. Some mutations in the BRAF gene including V600E result in constitutively activated BRAF proteins, which can cause cell proliferation in the absence of growth factors that would normally be required for proliferation. Vemurafenib is a selective inhibitor of the activated BRAFV600E gene, a gene found in 70% of malignant melanomas and a significant percentage of other cancers. It is speicfically indicated for the treatment of unresectable or metastatic melanoma with BRAFV600E mutation, as detected by an FDA-approved test. It is supplied as a tablet for oral administration. The recommended dose is 960 mg (four 240 mg tablets) twice daily. The first dose should be taken in the morning and the second dose should be taken in the evening approximately 12 hours later. Each dose can be taken with or without a meal. If a dose is missed, it can be taken up to four hours prior to the next dose to maintain the twice daily regimen. Both doses should not be taken at the same time
Everolimus: It is an inhibitor of mammalian target of rapamycin (mTOR). mTOR is a serine/threonine protein kinase that regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, and transcription. The mTOR pathway is dysregulated in several human cancers. Inhibition of mTOR by everolimus has been shown to reduce cell proliferation, angiogenesis, and glucose uptake in in vitro and/or in vivo studies. Everolimus is specifically approved for the treatment of progressive neuroendocrine tumors of pancreatic origin in patients with unresectable, locally advanced or metastatic disease. Everolimus is supplied as a tablet for oral administration. The recommended dose of Everolimus for pancreatic cancer is is 10 mg once daily
Sunitinib: An oral multi-kinase inhibitor and works by blocking multiple molecular targets implicated in the growth, proliferation and spread of cancer. Two Sunitinib targets, vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR), are expressed by many types of solid tumors and are thought to play a crucial role in angiogenesis, the process by which tumors acquire blood vessels, oxygen and nutrients needed for growth. Sunitinib also inhibits other targets important to tumor growth, including KIT, FLT3 and RET. Sunitinib is specifically indicated for the treatment of progressive, well-differentiated pancreatic neuroendocrine tumors in patients with unresectable locally advanced or metastatic disease. Sunitinib is supplied as a tablet for oral administration. The recommended dose for pancreatic meuroendocrine tumors is 37.5 mg taken orally once daily continuously without a scheduled off-treatment period.
Linagliptin: It is a newer orally-active inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme similar to sitagliptin and is approved for type 2 diabetes mellitus. Major adverse effect of this drug include nasopharyngitis, hypoglycemia and pancreatitis
Fidaxomicin: It is a narrow-spectrum macrocyclic antibiotic and is bactericidal against C. difficile in vitro. It acts by inhibiting RNA synthesis by RNA polymerases. Fidaxomicin is specifically indicated in adults for treatment of Clostridium difficile-associated diarrhea. To reduce the development of drug-resistant bacteria and maintain the effectiveness of Fidaxomicin, it should be used only to treat infections that are proven or strongly suspected to be caused by Clostridium difficile. Fidaxomicin is supplied as a tablet designed for oral administration. The recommended dose is one 200 mg tablet orally twice daily for 10 days with or without food. It can cause gastrointestinal hemorrhage, anemia and neutropenia.
Telaprevir and Boceprevir: These inhibits the hepatitis C protease NS3-4A, an enzyme that is essential for HCV viral replication. Telaprevir is specifically indicated, in combination with peginterferon alfa and ribavirin, for the treatment of genotype 1 chronic hepatitis C (CHC) in adults with compensated liver disease, including cirrhosis, who are treatment-naïve or who have been previously treated with interferon-based treatment, including prior null responders, partial responders, and relapsers. It is supplied as a tablet for oral administration.
Brentuximab vedotin: It is a CD30-directed antibody-drug conjugate (ADC) consisting of three components: 1) the chimeric IgG1 antibody cAC10, specific for human CD30, 2) the microtubule disrupting agent monomethyl auristatin E (MMAE) and 3) a protease-cleavable linker that covalently attaches MMAE to cAC10. Brentuximab vedotin is designed to be stable in the bloodstream, but to release MMAE upon internalization into CD30-expressing tumor cells, resulting in a targeted cell-killing effect. It is specifically approved for 1) Hodgkin lymphoma after failure of autologous stem cell transplant (ASCT) or after failure of at least two prior multi-agent chemotherapy regimens in patients who are not ASCT candidates and 2) systemic anaplastic large cell lymphoma after failure of at least one prior multi-agent chemotherapy regimen. It is supplied as a solution for intravenous infusion. The recommended dose is 1.8 mg/kg administered only as an intravenous infusion over 30 minutes every three weeks
Ruxolitinib: Is a kinase inhibitor and inhibits Janus Associated Kinases (JAKs) JAK1 and JAK2, which mediate the signaling of a number of cytokines and growth factors that are important for hematopoiesis and immune function. JAK signaling involves recruitment of STATs (signal transducers and activators of transcription) to cytokine receptors, activation and subsequent localization of STATs to the nucleus leading to modulation of gene expression. Myelofibrosis is a myeloproliferative neoplasm known to be associated with dysregulated JAK1 and JAK2 signaling. Ruxolitinib is specifically approved for intermediate or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia vera myelofibrosis and post-essential thrombocythemia myelofibrosis. Ruxolitinib is supplied as a tablet for oral administration. The recommended initial dose is based on platelet count. A complete blood count (CBC) and platelet count must be performed before initiating therapy, every 2 to 4 weeks until doses are stabilized, and then as clinically indicated. Anemia and thrombocytopenia are adverse effects.
Indacaterol: Is a long-acting beta2-adrenergic agonist. When inhaled, indacaterol acts locally in the lung as a bronchodilator. It is specifically approved for the treatment of airflow obstruction in patients with chronic obstructive pulmonary disease, including chronic bronchitis and/or emphysema.
Rilpivirine: A newer non-nucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus type 1 (HIV-1) similar to etravirine.
Belatacept: It is a a selective T-cell (lymphocyte) costimulation blocker. It binds to CD80 and CD86 on antigen-presenting cells, thereby blocking CD28 mediated costimulation of T lymphocytes. Activated T lymphocytes are the predominant mediators of immunologic rejection. Without immunosuppression, the body can reject a transplanted organ because the immune system recognizes the new organ as foreign. It is specifically indicated for the prophylaxis of organ rejection in adult patients receiving a kidney transplant. It is approved for use in combination with basiliximab induction, mycophenolate mofetil, and corticosteroids.
Tocilizumab: It is a recombinant humanized anti-human interleukin 6 (IL-6) receptor monoclonal antibody of the immunoglobulin IgG1 (gamma 1, kappa) subclass. Tocilizumab binds specifically to both soluble and membrane-bound IL-6 receptors and has been shown to inhibit IL-6-mediated signaling through these receptors. IL-6 is a pleiotropic pro-inflammatory cytokine produced by a variety of cell types including T- and B-cells, lymphocytes, monocytes and fibroblasts. IL-6 is also produced by synovial and endothelial cells leading to local production of IL-6 in joints affected by inflammatory processes such as rheumatoid arthritis. Tocilizumab is specifically indicated for the treatment of active systemic juvenile idiopathic arthritis in patients two years of age and older
Ezogabine: It is a potassium channel agent. The mechanism of its therapeutic effects has not been fully elucidated. In vitro studies indicate that it enhances transmembrane potassium currents mediated by the KCNQ family of ion channels. By activating KCNQ channels, It is thought to stabilize the resting membrane potential and reduce brain excitability. It is specifically indicated as adjunctive treatment of partial-onset seizures in adults.
Vilazodone hydrochloride: Is a selective serotonin reuptake inhibitor and a 5HT1A receptor partial agonist. The mechanism of the antidepressant effect of vilazodone is not fully understood. It is specifically indicated for the treatment of major depressive disorder.
Vandetanib: An orally available receptor tyrosine kinase (RTK) inhibitor, which blocks both the vascular endothelial growth factor (VEGF) RTK and the Epidermal Growth Factor (EGF) RTK. Blockade of the VEGF receptors limits the growth of new blood vessels, which are vital to supporting the growth of tumors. Without sufficient blood supply, tumor cells become starved for nutrients, slowing or halting growth. Vandetanib is specifically indicated for the treatment of symptomatic or progressive medullary thyroid cancer in patients with unresectable locally advanced or metastatic disease.
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