Review of Pharmacology - 9E (2015)

CHAPTER
19
New Drugs
1. Abatacept: Co-stimulation inhibitor useful for the treatment of DMARD resistant rheumatoid arthritis.
2. Abiraterone acetate: It is converted in vivo to abiraterone, an androgen biosynthesis inhibitor that inhibits 17
α-hydroxylase/C 17, 20-lyase (CYP17) It is indicated in combination with prednisone for the treatment of patients with
metastatic castration-resistant prostate cancer who have received prior chemotherapy containing docetaxel.
3. AbobotulinumtoxinA: An acetylcholine release inhibitor and a neuromuscular blocking agent for the treatment of
cervical dystonia in adults to reduce the severity of abnormal head position and neck pain, and for the temporary
improvement in the appearance of moderate to severe glabellar lines.
4. Acetyl-carnitine: Apart from increasing the cholinergic transmission, it also possesses antioxidant property It is useful in
slowing the progression of Alzheimer’s disease.
5. Aclidinium bromide: An anticholinergic with specificity for muscarinic receptors. It has similar affinity to the subtypes
of muscarinic receptors M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3 receptor at
the smooth muscle leading to bronchodilation. It has been recently approved for COPD.
6. Ado-trastuzumab emtansine: It is a HER2-targeted antibody (trastuzumab) and microtubule inhibitor (mertansine)
conjugate indicated for the treatment of patients with HER2-positive, metastatic breast cancer. Trastuzumab alone stops
growth of cancer cells by binding to the HER2/neu receptor, whereas mertansine enters cells and destroys them by
binding to tubulin. Because the monoclonal antibody targets HER2, and HER2 is only over-expressed in cancer cells, the
conjugate delivers the toxin specifically to tumor cells. Its major adverse effects include hepatotoxicity, cardiotoxicity
(reduction in left ventricular ejection fraction), and teratogenicity.
7. Afatinib: It is a tyrosine kinase inhibitor of EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4). It is specifically indicated
for the first-line treatment of patients with metastatic non-small cell lung cancer whose tumors have epidermal growth
factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test.
8. 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 It is
specifically approved for neovascular (wet) age-related macular degeneration.
9. Alcaftadine: It is a topical H1 histamine receptor antagonist indicated for the prevention of itching associated with
allergic conjunctivitis as an ophthalmic solution.
10. Aldesleukin: Recombinant 1L-2 useful for renal cell carcinoma and malignant melanoma.
11. Alefacept: Fusion protein against LFA- used for plaque psoriasis.
12. Alemtuzumab: Monoclonal antibody against CD 2 useful for B-cell CLL.
13. Aliskiren, Remikiren and Enalkiren: Oral renin inhibitors useful for the treatment of hypertension.
14. Alogliptin: It is a dipeptidyl peptidase-4 (DPP-4) inhibitor (like sitagliptin and vildagliptin) for the treatment of type 2
diabetes.
15. Alosetron: 5-HT3 antagonist used to reduce pain and diarrhoea in irritable bowel syndrome.
16. Altretamine: Anticancer drug useful for ovarian carcinoma.
17. Alvimopan: Peripheral µ opioid receptor antagonist useful for postoperative paralytic ileus.
18. Amineptine: Serotonin reuptake enhancer similiar to tianeptin for depression.
19. Anakinra: Inhibitor of 1L-1 useful in septic shock and rheumatoid arthritis.
20. Anecorvate: Angiogenesis inhibitor for neovascular age related macular degeneration.
21. Apafant and Lexipafant: PAF antagonists being investigated for the treatment of acute pancreatitis.
22. Apixaban: A factor Xa inhibitor anticoagulant indicated to reduce the risk of stroke and systemic embolism in patients
with non-valvular atrial fibrillation.
23. Aprepitant: Neurokinin NK1 (substance P) receptor antagonist useful for the treatment of chemotherapy induced
vomitting.
24. Asenapine: An atypical antipsychotic used sublingually for the treatment of schizophrenia and acute mania or mixed
episodes associated with bipolar I disorder.
25. Asoprisnil: Selective progesterone receptor modulator being tried for leiomyoma.
26. Atosiban: Oxytocin receptor antagonist used to delay premature labour.
27. Avanafil: It is a phosphodiesterase 5 (PDE5) inhibitor like sildenafil and is specifically indicated for the treatment of
erectile dysfunction.
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