Drug intelligence / Profile preview

capecitabine + yttrium-90 resin microspheres

Development stage
Phase 1
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Small Molecules
Administration
Oral, Intra-arterial
01

Overview

Capecitabine + yttrium-90 resin microspheres is a combination therapy used primarily for the treatment of advanced or unresectable liver-dominant cancers, including metastatic colorectal cancer and intrahepatic cholangiocarcinoma. Capecitabine is an oral prodrug of 5-fluorouracil (5-FU), a small molecule antimetabolite that inhibits DNA synthesis by interfering with thymidylate synthase activity in rapidly dividing tumor cells. Yttrium-90 (Y-90) resin microspheres are radiolabeled beads administered via selective internal radiation therapy (SIRT), also known as radioembolization. These microspheres deliver targeted beta radiation directly to hepatic tumors through the arterial blood supply, maximizing tumoricidal effects while sparing healthy liver tissue. The combination leverages the radiosensitizing properties of capecitabine to enhance the efficacy of localized radiotherapy delivered by Y-90 microspheres. Clinical studies have shown this regimen to be generally well tolerated, with manageable toxicity profiles and encouraging clinical activity in patients with unresectable or chemotherapy-refractory liver metastases from colorectal cancer[1][3][4]. The most common adverse events include mild hematologic toxicity, transient transaminitis, nausea, abdominal pain, fatigue, and hand-foot syndrome[1].

Other names
capecitabine plus yttrium-90 resin microspherescapecitabine and Y-90 SIR-Spherescapecitabine with selective internal radiation therapy
02

Targets

TS (Thymidylate synthase)

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