27.01.2023

Effective drugs in prostate cancer

The treatment of prostate cancer is aimed at achieving remission, gaining control over the disease and preventing complications.

Drugs for prostate cancer in each case selected individually, depending on the stage, comorbidities, aggressiveness of the tumor, age of the patient.

Use the following medicines:

  • Gonadotropin-releasing hormone agonists;
  • Antagonists androgens;
  • Estrogens (rarely).
  • Bisphosphonates;
  • Chemotherapeutic agents;
  • Corticosteroids;
  • Antifungal;
  • Immunological preparations;
  • Anticancer.
Agonists of luteinizing hormone releasing hormone

Agonists gonadotropin-releasing hormone used for medical castration in patients with prostate cancer.

Indications:

  • localized prostate cancer (if it is not possible to perform radical treatment or as neoadjuvant measures before surgery or radiation therapy);
  • locally advanced cancer without metastasis as a single agent or neoadjuvant and adjuvant therapy in combination with surgery and or light;
  • metastatic prostate cancer.

They act on the gonadotropin-producing cells of the pituitary gland, stimulating the synthesis of luteinizing hormone (LH) and follicle stimulating hormone (FSH) and, consequently, increase the testosterone level in a few weeks. Prior to the introduction of agonists prescribe antiandrogens to block the effect of testosterone on prostate cells.

When using drugs within 3-5 weeks of LH and FSH decrease, along with testosterone, to the threshold level of castration (50 NG/DL).

Representative – Leuprorelin (Eligard, Lupron-Depot, Depot-PED).

Leuprorelin is indicated as palliative treatment for progressive prostate cancer, when orchiectomy or the use of estrogen is not applicable for the patient. It is also a potent inhibitor of gonadotropin secretion during continuous treatment at therapeutic doses.

Leuprorelin can be used as a depot in a dose of 3.75 mg every 4 weeks 11.25 mg every 12 weeks, or 30 mg every 24 weeks. Lupron should be administered intramuscularly, subcutaneously and Eligard.

Triptorelin (Diphereline,Trelstar, Trelstar Mixject)

Triptorelin is indicated for the treatment of symptomatic progressive hormone-dependent prostate cancer, metastatic and localized forms (alternative to surgical castration to suppress testosterone secretion). The recommended dosage 3.75 mg intramuscularly every 4 weeks, of 11.25 mg intramuscularly every 12 weeks or 22.5 mg intramuscularly every 24 weeks.

Triptorelin is a synthetic Decapeptide agonist analogue of GnRH. It reduces the secretion of LH and FSH, and consequently, reduces the levels of testosterone and estrogen. The concentration of testosterone in the background of the drug reaches the post-castration levels after 3 weeks.

Another drug with similar action and indications – Goserelin (Zoladex)

Dosage: 3.6 mg and 10.8 mg subcutaneous implant. The standard dose is 3.6 mg every 4 weeks or 10.8 mg every 12 weeks.

The reduction in testosterone production leads to a decrease in the size of the prostate and reduces associated symptoms.

Histrelin (Vantas, Supprelin)

The drug is administered in an amount of 50 mg as a subcutaneous implant designed to provide continuous release histrelin a nominal rate of 50-60 mcg/day over 12 months. The recommended dose of 1 subcutaneous implant every 12 months.

Histrelin – a potent inhibitor of gonadotropin secretion.

Some experts recommend the use of agonists Lgrg intermittent course, but the effectiveness of the scheme is not proven.

Therapy designed for a long period, before the onset of refractoriness to hormones.

Antiandrogens

For prostate cancer the positive therapeutic effect of antiandrogens that bind to androgen receptors and competitively inhibit their interaction with testosterone and dihydrotestosterone. As a single agent is ineffective.

Allocate clean and steroid antiandrogens.

Preferable non-steroidal or pure antiandrogens because they selectively interact with their receptors in the prostate and not have antigonadotropnym mechanism. In addition, there is a blocking of androgen receptors in the hypothalamus, in the locus, where is the development Lnrg. Due to the existing feedback mechanism in the synthesis of LH increases which leads to higher levels of testosterone (a temporary condition).

When castrate-refractory prostate cancer do not apply.

Abiraterone (Abiraterone, Zytiga)

Abiraterone administered in combination with Prednisone for the treatment of patients with metastatic castrate-resistant prostate cancer during or after chemotherapy (Docetaxel).

The dosage is 1000 mg once daily in combination with Prednisone 5 mg twice a day.

Abiraterone is an inhibitor of the biosynthesis of androgens.

Bicalutamide (Casodex)

Bicalutamide is indicated for the treatment of metastatic prostate cancer in combination with an agonist of LHRH. The standard dosage is 50 mg orally 1 time in the morning or evening.

Degarelix ( Degarelix, Firmagon, Firmagon)

Degarelix – selective antagonist pituitary GnRH-receptors, reduces production of gonadotropins, LH and FSH, thereby testosterone produced less.

Indications for use – advanced hormone-dependent prostate cancer.

Degarelix effective for achieving and maintaining testosterone on post-castration level. Unlike the GnRH agonists, causes a short-term increase in testosterone levels; the desired effect is achieved within 1-3 days of receipt.

The initial dose is 240 mg, administered subcutaneously (2 injections of 120 mg at a concentration of 40 mg / ml). The maintenance dose is 80 mg subcutaneously (at a concentration of 20 mg/ml) every 28 days. The first maintenance dose is administered after 28 days after start of treatment.

Flutamid

Flutamide used in combination with GnRH agonists for the management of locally-limited cancer at an early stage and to treat metastatic cancer, for patients with bilateral orchiectomy. Usual dosage is – 250 mg every 8 hours.

Nilutamid (Nilutamid, Nilandron)

Nilutamid not suitable for induction of chemical castration, because, by blocking the feedback mechanism for control of testosterone secretion, it increases its concentration. The drug is used in combination with surgical castration for treatment of metastatic cancer of the prostate, the presence or absence of a local process, in combination with surgical or pharmacological castration.

Initial dose 300 mg 1 times a day, 30 days, maintenance dose for nilutamide is 150 mg once a day.

Insulated (Enzalutamide, Xtandi)

Palliative treatment of malignant tumor of the prostate with metastases.

Apartame (Apalutamid, Erleada)

Apartame inhibits nuclear translocation of the androgen receptor, DNA binding and prevents its transcription.

Indications: therapy nemetstaticescoy hormone-resistant prostate cancer.

Anticancer drugs
Docetaxel (Docetaxel, Docefrez, Taxotere)

Docetaxel is indicated in combination with Prednisone for the treatment of patients with androgen-independent metastatic prostate cancer. The usual dose is 75 mg/m2 every 3 weeks as 1-hour infusion, with Prednisone 5 mg orally twice a day.

Cabazitaxel (Сabazitaxel, Jevtana)

Cabazitaxel prescribed with Prednisone to treat metastatic prostate cancer after chemotherapy with Docetaxel.

The standard dosage is 25 mg/m2, administered as an intravenous infusion every 3 weeks in combination with prednisone 10 mg daily for treatment cabazitaxel. Reduce the dose to 20 mg / m2 if patients develop adverse reactions.

Mitoxantrone

For patients who oncobasidium with recommended symptomatic treatment, and which do not apply therapy with Docetaxel, Mitoxantrone, as a palliative means, improves the quality of life, but does not affect its duration.

The drug is prescribed in combination with corticosteroids.

The recommended dose is 12-14 mg / m2, intravenous infusion of 1 every 21 days.

Estramustin (Estracyt, Estramustin, Emcyt)

Estramustin – antineoplastic hormonal agent that contains estradiol and mechlorethamine.

Mechanisms of action:

  • antiandrogenic;
  • estrogen;
  • antigonadotropnym;
  • anticancer;
  • cytostatic.

Used in combination with Vinblastine, Etoposide, Paclitaxel, Docetaxel, Mitoxantrone, or corticosteroids to achieve synergistic effects.

Estramustin, is indicated for the palliative treatment of metastatic and/or progressive prostate cancer, especially hormoneproducing tumors.

The average dosage of 14 mg / kg per day in 3-4 reception. Treatment can begin with intravenously injections for 300/450 mg 1 time a day for 3 weeks and then switch to oral use 280-420 mg or intravenous injection at 300 mg 2 times per week.

If within one month there is no positive dynamics, drug overturned.

Immunopreparat in prostate cancer

Autologous cellular immunotherapy that stimulates an immune system of the patient to fight the cancer.

It is tested the first vaccine of the second generation against a malignant tumor of the prostate. On the progression of the tumor Provenge is not affected, but is able to increase life expectancy. According to scientists, the vaccine is safe and can be used at any stage of the guidance, including for the palliative treatment of tumors resistant to standard hormonal therapy. The appearance of pronounced pain syndrome the vaccine is not prescribed. Treatment for each individual patient.

Obstacle to the massive purpose – high cost.

Derivatives Bisphosphonate

In men with prostate cancer and bone metastases zoledronic acid is prescribed to prevent or delay disease-associated bone resorption.

In prostate cancers with distant metastases are often complicated by fractures or spinal cord compression. When these complications discusses the question of surgical intervention or radiation therapy.

Zoledronic acid (zometa)

Zoledronic acid is an intravenous bisphosphonate that is indicated for patients with proven bone metastases after standard chemotherapy.

Intravenous administration of 4 mg every 3 or 4 weeks. The treatment is controlled by the level of creatinine.

The duration of 9-15 months. Additionally, the recommended intake of calcium 500 mg and vitamin complex containing vitamin D (400 IU per day).

Monoclonal antibody Denosumab (Prolia, Xgeva)

Monoclonal antibody (Denosumab) reduce the rate of complications (fractures, spinal cord compression, need for radiation therapy) in men with bone metastases from prostate cancer.

Denosumab – a genetically engineered drug based on monoclonal antibodies person.

Inhibiting the development and activity of osteoclasts, Denosumab decreases bone resorption and increases bone density.

The drug known under the brand name of Prolia (Prolia), shown to increase bone mass in the background of the use of antiandrogens about nemetstaticescoy prostate cancer.

The dose of 60 mg subcutaneously every 6 months.

Analog – Xgeva, the dosage of 120 mg subcutaneously every 4 weeks.

Patients should receive supplements of calcium 1000 mg and vitamin D 400 IU per day.

Corticosteroids

Corticosteroids have anti-inflammatory properties, used in prostate cancer metastasis that is not amenable to hormone therapy.

Corticosteroids modify the immune response, they are used in combination with Mitoxantrone, and Docetaxel Abiraterone.

Prednisone (Prednisone), Hydrocortisone (A-Hydrocort, Cortef, solu-cortef), and Dexamethasone

Prednisolone improves the condition and reduces the level of prostate specific antigen (PSA). Large doses can be used for patients with spinal cord compression or cerebral edema.

Low and medium doses of steroids suppress adrenal androgens. The symptomatic effect was observed in 60% of patients in the treatment of Dexamethasone at a dose of 0.75 mg 2 times a day.

Corticosteroids also exert a palliative effect in patients with prostate cancer and in pharmacological doses reduces the inflammation.

Radiopharmaceutical radium-223 dichloride (Xofigo, Cafego)

The drug is indicated for men with hormoneresistant prostate cancer and only bone metastases for the internal radiation therapy.

Increases the duration and quality of life.

In Russia, this method of treatment is limited.

Antifungal agents for prostate cancer

In high doses, Ketoconazole Nizoral inhibits adrenal and testicular production of male sex hormones due to the disintegration of the P450-dependent system.

Many side effects are somewhat offset by the simultaneous appointment of Prednisolone.

The effect of treatment with Ketoconazole, in contrast to the use of antiandrogens, is developing rapidly but is short-term.

Not all experts consider it appropriate treatment with Ketoconazole.

Victoria Mishina, urologist, medical columnist

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