Английская Википедия:Cabazitaxel

Материал из Онлайн справочника
Перейти к навигацииПерейти к поиску

Шаблон:Short description Шаблон:Use mdy dates Шаблон:Infobox drug

Cabazitaxel, sold under the brand name Jevtana, is a semi-synthetic derivative of a natural taxoid.[1] It is a microtubule inhibitor,[2] and the fourth taxane to be approved as a cancer therapy.Шаблон:Citation needed

Cabazitaxel was developed by Sanofi-Aventis and was approved by the U.S. Food and Drug Administration (FDA) for the treatment of hormone-refractory prostate cancer in June 2010.[3][4][5] It is available as a generic medication.[6][7]

Medical uses

Cabazitaxel is indicated in combination with prednisone for the treatment of metastatic castration-resistant prostate cancer following docetaxel-based treatment.[2]

Mechanism of action

Taxanes enhance microtubule stabilization and inhibit cellular mitosis and division.[8] Moreover, taxanes prevent androgen receptor (AR) signaling by binding cellular microtubules and the microtubule-associated motor protein dynein, thus averting AR nuclear translocation.[9]

Clinical trials

In patients with metastatic castration-resistant prostate cancer (mCRPC), overall survival (OS) is markedly enhanced with cabazitaxel versus mitoxantrone after prior docetaxel treatment. FIRSTANA (ClinicalTrials.gov identifier: NCT01308567) assessed whether cabazitaxel 20 mg/m2 (C20) or 25 mg/m2 (C25) is superior to docetaxel 75 mg/m2 (D75) in terms of OS in patients with chemotherapy-naïve mCRPC. However, C20 and C25 did not demonstrate superiority for OS versus D75 in patients with chemotherapy-naïve mCRPC. Cabazitaxel and docetaxel demonstrated different toxicity profiles, and C20 showed the overall lowest toxicity.[10] In a phase III trial with 755 men for the treatment of castration-resistant prostate cancer, median survival was 15.1 months for patients receiving cabazitaxel versus 12.7 months for patients receiving mitoxantrone. Cabazitaxel was associated with more grade 3–4 neutropenia (81.7%) than mitoxantrone (58%).[11] Common adverse effects with cabazitaxel include neutropenia (including febrile neutropenia) and GIT side effects appeared mainly in diarrhea, whereas, neuropathy was rarely detected.[12]

Pharmacokinetics

Cabazitaxel administration causes a decrease in plasma concentrations showing triphasic kinetics: a mean half life (t1/2) of 2.6 min in the first phase, a mean t1/2 of 1.3 h in the second phase, and a mean t1/2 of 77.3 h in the third phase.[13]

Metabolism

Cabazitaxel is basically metabolized in the liver by [cytochrome P450 (CYP)3A4/5 > CYP2C8], which result in seven plasma metabolites and excreted 20 metabolites. During 14 days after administration, 80% of cabazitaxel is excreted: 76% in the feces and 3.7% as a renal excretion.[14]

References

Шаблон:Reflist

External links

Шаблон:Chemotherapeutic agents Шаблон:Portal bar

Партнерские ресурсы
Криптовалюты
Магазины
Хостинг
Разное

  1. ↑ Шаблон:Cite web
  2. ↑ 2,0 2,1 Ошибка цитирования Неверный тег <ref>; для сносок Jevtana FDA label не указан текст
  3. ↑ Шаблон:Cite web
  4. ↑ Шаблон:Cite press release
  5. ↑ Шаблон:Cite press release
  6. ↑ Шаблон:Cite web
  7. ↑ Шаблон:Cite web
  8. ↑ Шаблон:Cite journal
  9. ↑ Шаблон:Cite journal
  10. ↑ Шаблон:Cite journal
  11. ↑ Шаблон:Cite webШаблон:Dead link
  12. ↑ Шаблон:Cite journal
  13. ↑ Шаблон:Cite journal
  14. ↑ Шаблон:Cite journal
Источник — http://wikihandbk.com/ruwiki/index.php?title=Английская_Википедия:Cabazitaxel&oldid=13718823