Drug intelligence / Profile preview

apatinib + capecitabine + paclitaxel

Development stage
Unknown
Lead developer
Roche
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

The combination of apatinib, capecitabine, and paclitaxel is a multi-drug regimen used primarily in cancer treatment. This combination brings together three distinct medications with complementary mechanisms of action. Apatinib is a novel antiangiogenic drug that works by inhibiting vascular endothelial growth factor receptor-2 (VEGFR-2), which plays a crucial role in tumor angiogenesis[1][4]. Capecitabine is an oral fluoropyrimidine that converts to 5-fluorouracil in tumor tissues, interfering with DNA synthesis and cell division[2][3]. Paclitaxel is a taxane that promotes microtubule assembly and stability, preventing cell division and leading to cell death[7][10]. This combination therapy has been studied in various cancer types, including metastatic breast cancer, esophageal squamous cell carcinoma, and biliary tract cancer[1][5][9]. Clinical evidence suggests that this combination shows promising efficacy with manageable toxicity profiles. ## Clinical Applications **Metastatic Breast Cancer** The combination has been explored in patients with metastatic breast cancer who failed to respond to multifaceted therapy. In one study, 12 patients received apatinib combined with capecitabine, while 19 patients received apatinib combined with taxane drugs[5]. The initial dose of apatinib was typically 250 mg/day, with adjustments made based on tolerability. **Esophageal Squamous Cell Carcinoma** For patients with esophageal squamous cell carcinoma who had failed first-line chemotherapy, apatinib combined with various agents including capecitabine and paclitaxel has demonstrated promising outcomes[1]. These combinations have shown potential as effective second-line treatment options. **Biliary Tract Cancer** A phase 2 study investigated a similar combination (camrelizumab, apatinib, and capecitabine) in patients with advanced biliary tract cancer, showing promising antitumor activity and manageable toxicity, particularly in the first-line setting[9]. ## Safety Profile The safety profile of this combination therapy is generally described as tolerable, though dose adjustments may be necessary. Common adverse events include: - Elevated liver enzymes (gamma-glutamyltransferase, aspartate aminotransferase, alanine aminotransferase)[1] - Hematological toxicities (thrombocytopenia)[9] - Hand-foot syndrome (associated with capecitabine) - Fatigue - Nausea In some studies, the initial dose of apatinib was reduced from 250 mg/day to 250 mg every second day in certain patients due to intolerable adverse events[5]. This highlights the importance of individualized dosing based on patient tolerability. The combination therapy represents an emerging approach in cancer treatment, particularly for patients who have progressed on or are intolerant to standard first-line therapies. Its efficacy and safety continue to be evaluated in various clinical settings.

02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)TUBB (Tubulin (alpha and beta subunits))TS (Thymidylate synthase)

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