II. Indications
- Adjuvant Chemotherapy (FDA approved)
- Colorectal Cancer (including metastatic cancer)
- Metastatic Breast Cancer
- Off-Label Use (non-FDA approved)
- Gastrointestinal Cancer (Gastric Cancer, Esophageal Cancer, Pancreatic Cancer, Hepatobiliary cancer, Anal Cancer)
- Gynecologic Cancer (Ovarian Cancer, Fallopian tube cancer, peritoneal cancer)
- Neuroendocrine Tumors
III. Contraindications
- Creatinine Clearance <30 ml/min
IV. Mechanism
- Antimetabolite Chemotherapy (Antineoplastic Agent)
- Fluoropyrimidine Carbamate, acts as a prodrug
- Selectively activated by tumor cells to 5-Fluorouracil (5-FU)
-
5-Fluorouracil (5-FU) is further metabolized by normal cells and tumor cells to 2 active agents
- 5-fluoro-2-deoxyuridine monophosphate (FdUMP)
- Decreases thymidine synthesis
- Inhibits DNA synthesis and cell division
- 5-fluorouridine triphosphate (FUTP)
- Competes with Uridine Triphosphate for incorporation into RNA
- Inhibits RNA and Protein synthesis
- 5-fluoro-2-deoxyuridine monophosphate (FdUMP)
V. Dosing
- See other references for disease specific dosing protocols
VI. Adverse Effects
- Cardiovascular (cardiac toxicity, esp in Overdose)
- Endo
- Impaired future fertility
- Gastrointestinal
- Mucositis
- Severe Diarrhea
- Hyperbilirubinemia
- Typhlitis (RLQ Pain in neutropenic patients)
- Hematologic
- Myelosuppression (peaks at 1 week after dose)
- Neuro
- Headache
- Palmar-Plantar erythrodysesthesia (sensory Neuropathy)
- Encephalopathy
- Skin
- Acral swelling and erythema (hand and foot syndrome)
- Alopecia
VII. Pharmacokinetics
- Oral Bioavailability: 40 to 60%
- Peak serum concentration: 2 hours
- Catabolized by dihydropyrimidine dehydrogenase (DPD) into inactive metabolite
- Variable metabolism in DPD deficiency
- Inactive metabolite excreted in the urine
VIII. Safety
- Avoid in Pregnancy (any trimester)
- Use reliable Contraception
- Avoid in Lactation
- Monitoring
IX. Drug Interactions
- Capecitabine increases level of other drugs
-
Antacids
- Increase Capecitabine levels
-
Allopurinol
- Avoid with Capecitabine
X. Management: Toxicity or Overdose
- Evaluation
- Complete Blood Count (repeated several days after dose)
- Comprehensive metabolic panel
- Consider serum Troponin
- Electrocardiogram (EKG)
- Acute ingestion
- Consider Activated Charcoal
- Indicated if <1 hour after ingestion and intact mentation
- Consider Uridine Triacetate 10 g
- Indicated in severe toxicity or acute Overdose >2 g
- Consider Activated Charcoal
- Other supportive measures
- Intravenous Fluids
- Granulocyte colony stimulation factors if significant myelosuppression
- Disposition
- Patients with mild gastrointestinal symptoms after therapeutic dose may be discharged
- Observe patients with severe symptoms or intentional Overdose
XI. Resources
- Capecitabine Tablet (DailyMed)
XII. References
- Tomaszewski (2024) Crit Dec Emerg Med 38(2): 34
Images: Related links to external sites (from Bing)
Related Studies
capecitabine (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
CAPECITABINE 500 MG TABLET | Generic | $0.56 each |
Ontology: capecitabine (C0671970)
Definition (NCI_NCI-GLOSS) | A drug used to treat stage III colon cancer in patients who had surgery to remove the cancer. It is also used to treat metastatic breast cancer that has not improved after treatment with certain other anticancer drugs. Xeloda is being studied in the treatment of other types of cancer. It is taken up by cancer cells and breaks down into 5-fluorouracil, a substance that kills tumor cells. Xeloda is a type of antimetabolite. |
Definition (NCI) | A fluoropyrimidine carbamate belonging to the class of antineoplastic agents called antimetabolites. As a prodrug, capecitabine is selectively activated by tumor cells to its cytotoxic moiety, 5-fluorouracil (5-FU); subsequently, 5-FU is metabolized to two active metabolites, 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP) by both tumor cells and normal cells. FdUMP inhibits DNA synthesis and cell division by reducing normal thymidine production, while FUTP inhibits RNA and protein synthesis by competing with uridine triphosphate for incorporation into the RNA strand. (NCI04) |
Definition (PDQ) | A fluoropyrimidine carbamate belonging to the class of antineoplastic agents called antimetabolites. As a prodrug, capecitabine is selectively activated by tumor cells to its cytotoxic moiety, 5-fluorouracil (5-FU); subsequently, 5-FU is metabolized to two active metabolites, 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP) by both tumor cells and normal cells. FdUMP inhibits DNA synthesis and cell division by reducing normal thymidine production, while FUTP inhibits RNA and protein synthesis by competing with uridine triphosphate for incorporation into the RNA strand. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42852&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42852&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1794" NCI Thesaurus) |
Concepts | Pharmacologic Substance (T121) , Nucleic Acid, Nucleoside, or Nucleotide (T114) |
MSH | C110904 |
SnomedCT | 108761006, 386906001 |
English | 5'-Deoxy-5-fluoro-N-[(pentyloxy)carbonyl]-cytidine, N(4)-pentyloxycarbonyl-5'-deoxy-5-fluorocytidine, capecitabine (medication), CAPECITABINE, capecitabine [Chemical/Ingredient], Capecitabine (product), Capecitabine (substance), Capecitabine, CAPE, capecitabine |
Spanish | capecitabina (producto), capecitabina (sustancia), capecitabina |