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Targeted Drug Therapy for Osteosarcoma

In recent years, new drugs that target specific parts of cancer cells have been developed (targeted drugs). They can be used along with chemo in some situations. Or, if chemo drugs are no longer helpful, targeted drugs might be an option.

Tyrosine kinase inhibitors (TKI)

TKIs work by blocking the signals cells need to grow and divide. Specifically, these drugs affect a tumor’s ability to grow new blood vessels, which it needs to grow and survive. Some examples of TKIs that have been tried in osteosarcoma include:

  • Regorafenib (Stivarga)
  • Sorafenib (Nexavar)
  • Cabozantinib (Cabometyx)

Other TKIs are currently being studied for use in osteosarcoma treatment.

Possible side effects

Side effects of these drugs can include fatigue, loss of appetite, hand-foot syndrome (redness and irritation of the hands and feet), high blood pressure, weight loss, diarrhea, and abdominal (belly) pain.

Less common but more serious side effects can include problems with blood flow to the heart, bleeding, abnormal thyroid test results, and perforations (holes) in the stomach or intestines.

More information about targeted therapy

To learn more about how targeted drugs are used to treat cancer, see Targeted Cancer Therapy.

To learn about some of the side effects listed here and how to manage them, see Managing Cancer-related Side Effects.

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Developed by the American Cancer Society medical and editorial content team with medical review and contribution by the American Society of Clinical Oncology (ASCO).

Anderson ME, Dubois SG, Gebhart MC. Chapter 89: Sarcomas of bone. In: Niederhuber JE, Armitage JO, Doroshow JH, Kastan MB, Tepper JE, eds. Abeloff’s Clinical Oncology. 6th ed. Philadelphia, Pa: Elsevier; 2020.

Gill J, Gorlick R. Advancing therapy for osteosarcoma. Nat Rev Clin Oncol. 2021;18(10):609-624.

Italiano A, Mir O, Mathoulin-Pelissier S, et al. Cabozantinib in patients with advanced Ewing sarcoma or osteosarcoma (CABONE): a multicentre, single-arm, phase 2 trial. Lancet Oncol. 2020;21(3):446-455.

Janeway K, Randall R, Gorlick R. Chapter 28: Osteosarcoma. In: Blaney SM, Adamson PC, Helman LJ, eds. Pizzo and Poplack’s Pediatric Oncology. 8th ed. Philadelphia Pa: Lippincott Williams & Wilkins; 2021.

National Cancer Institute. Osteosarcoma and Undifferentiated Pleomorphic Sarcoma of Bone Treatment (PDQ). 2024. Accessed at https://www.cancer.gov/types/bone/hp/osteosarcoma-treatment-pdq on June 3, 2025.

National Comprehensive Cancer Network (NCCN). Practice Guidelines in Oncology: Bone Cancer. Version 2.2025. Accessed at www.nccn.org/professionals/physician_gls/pdf/bone.pdf on June 3, 2025.

Last Revised: August 21, 2025

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