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Posts Tagged ‘Conjugated’

Estramustine Phosphate Sodium

Posted by admin on June 24th, 2011 No Comments
C23H30ClNNaO6P • Estramustine phosphate sodium, a complex of 17 ?-estradiol and nornitrogen mustard, is an antimicrotubule antineoplastic agent. Uses • Prostate Cancer Estramustine phosphate sodium is used for the palliative treatment of metastatic and/or progressive prostate cancer. The drug, alone or in combination with other antineoplastic agents, currently is considered by many clinicians to be an alternative to conventional measures (e.g., orchiectomy, hormonal therapy) and generally is used in the treatment of hormone-refractory prostate cancer. Safety and efficacy of estramustine have been evaluated in controlled and uncontrolled studies in patients with advanced metastatic prostate cancer refractory to conventional measures (e.g., hormonal therapy) as well as in those with previously untreated disease. Most studies were conducted before the realization that administration of estramustine with milk or calcium-containing products substantially impairs absorption of the drug; therefore, overall clinical efficacy (i.e., objective response) of estramustine may have been underestimated. Read more [...]
Posted in Drugs

Progesterones and Estrogens

Posted by admin on June 21st, 2011 No Comments
Megestrol acetate has several mechanisms of action that suggest a potential beneficial role in treating progressive metastatic prostate cancer. It inhibits the release of luteinizing hormone, 5 a-reductase conversion of testosterone to dihydrotestosterone, binding of androgen to its receptor, and at high doses may be cytotoxic. Based on clinical reports that suggest a dose-response effect, Dawson et al. studied two doses for the CALGB (160 mg versus 640 mg). The prostate-specific antigen response was only 12%, however, with no dose effect and no association with prior response to antiandrogen withdrawal. An unexpected tumor flare was observed in some patients, suggesting that megestrol acetate had agonistic activity. There was a similar low response rate reported in a smaller retrospective study. The palliative benefit of both estrogens and orchiec-tomy in the treatment of advanced prostate cancer was first reported in 1941, by Huggins and Hodges. In the setting of hormone-sensitive disease, the inhibitory effect of estrogen is due to suppression of pituitary gonadotropins and in turn testosterone. Read more [...]
Posted in Hormonal Therapy

Immunoconjugates

Posted by admin on May 6th, 2011 No Comments
Overview. Immunoconjugation is a means of delivering cytotoxic molecules to tumor cells. The effector molecules are attached to monoclonal antibodies (MAbs), which target the agent to specific antigens expressed on the tumor cell. When in circulation, the linkage between the effector molecule and antibody is stable, but, once inside the cell, it breaks down and the cytotoxic molecule is released, resulting in cell death. This method allows a higher concentration of the drug to be safely administered to the patient. This section focuses on MLN-2704, a form of the anti-PSMA (prostate-specific membrane antigen) MAb MLN-591 conjugated with DM1, and on MLN-591 RL, a second form of the same antibody conjugated with yttrium-90. Other MAbs in development include Medarex's MDX-010 (formerly MDX-101), a human MAb against cytotoxic T-lymphocyte antigen-4 (CTLA-4); Medarex's MDX-214, a human MAb specific to CD89; Medarex's MDX-070 (HuRx-Prostate), a human MAb against PSMA; Medlmmune' s Vitaxin, a humanized version of LM-609 that blocks the alpha-v / beta-3 integrin receptor (vit-ronectin) and thus inhibits Read more [...]
Posted in Prostate Cancer

Progesterone

Posted by admin on August 9th, 2010 No Comments
(British Approved Name, rINN) Drug Nomenclature International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish): Synonyms: Corpus Luteum Hormone; Luteal Hormone; Luteine; Luteohormone; NSC-9704; Pregnenedione; Progesteron; Progesterona; Progesteronas; Progesteroni; Progesteronum; Progeszteron BAN: Progesterone INN: Progesterone [rINN (en)] INN: Progesterona [rINN (es)] INN: Progestérone [rINN (fr)] INN: Progesteronum [rINN (la)] INN: Прогестерон [rINN (ru)] Chemical name: Pregn-4-ene-3,20-dione Molecular formula: C21H30O2 =314.5 CAS: 57-83-0 ATC code: G03DA04 Read code: y07kn; y07ko Pharmacopoeias. In China, Europe, International, Japan, US. European Pharmacopoeia, 6th ed. (Progesterone). Awhite or almost white crystalline powder or colourless crystals. It exhibits polymorphism. Practically insoluble in water freely soluble in dehydrated alcohol sparingly soluble in acetone and in fatty oils. Protect from light. The United States Pharmacopeia 31, 2008 (Progesterone). A white or creamy-white, odourless, crystalline powder. Practically Read more [...]
Posted in Drugs

Immunotherapies for Prostate Cancer

Posted by admin on July 19th, 2010 No Comments
Prostate cancer is the second leading cause of death in men, with approximately 220,000 new cases and an expected 28,000 deaths in the year 2003. A decrease in prostate cancer related deaths has been attributed to early prostate-specific antigen (PSA) detection, more effective chemotherapy treatments, and immunotherapies. Although tumors can often evade an immune response by modulating their tumor antigens, reducing major histocompatibility complex-1 (MHC-I) expression or inhibiting cytotoxic T-cell activity, the use of immune modulation for prostate cancer is a relatively new concept because the prostate is not generally considered a site where immune processes typically occur. Since tumors arise when cancer cells evade the immune system, the prostate is an ideal target for immunotherapy The four most common types of lesions associated with the prostate are acute/chronic prostatitis (bacterial/abacterial), proliferative inflammatory atrophy (PIA), benign prostatic hyperplasia (BPH), and prostate carcinoma. The types of proliferative lesions that occur in the prostate are in different regions Read more [...]
Posted in Pharmacotherapy

Plenaxis (Abarelix): drug for the treatment of advanced prostate cancer

Posted by admin on March 13th, 2010 No Comments
Trade Name Drug: Plenaxis Generic Name Drug: Abarelix Company: Praecis Pharmaceuticals Indication/Use: Prostate cancer Approval Date: Nov. 25, 2003 FDA Class: 1P Development Abarelix (Plenaxis) is an injectable decapeptide antagonist of leutinizing hormone­releasing hormone (LHRH) that was approved by the FDA in November 2003 for the treatment of advanced prostate cancer. Because of an increased risk of serious, and potentially life-threatening, allergic reactions associated with the use of abarelix, the drug will be marketed under a voluntary risk management program (RMP) intended to restrict distribution of the drug to patients with advanced prostate cancer who have no alternative therapy. About 5% to 10% of men with prostate cancer have the type of advanced, symptomatic disease that would make them candidates for abarelix therapy. The RMP for abarelix is called the PLUS (Plenaxis User Safety) Program. Carcinoma of the prostate is predominantly a tumor of older men, which frequently responds to treatment when widespread and may be cured when localized. The rate of tumor growth varies Read more [...]
Posted in Drugs

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