Targeted Therapy
What is targeted therapy?
Targeted therapy is the name for a group of medicines that precisely identify and treat specific types of breast cancer cells, such as cells that have too many HER2 proteins or have a BRCA mutation. Targeted therapy is a type of precision medicine — it uses information within or on the surface of cancer cells to precisely treat a specific type of breast cancer.
Many targeted therapy medicines fall into two classes: CDK4/6 inhibitors and anti-HER2 therapies.
CDK4/6 inhibitors treat hormone receptor-positive, HER2-negative breast cancer. They work by stopping cancer cells from dividing.
Anti-HER2 therapies treat all stages of HER2-positive breast cancer. They work by blocking the HER2 receptors that help the cancer grow.
Some targeted therapy medicines are antibodies that work like the antibodies made naturally by your immune system. These medicines may be called immune targeted therapy. They work by helping your immune system recognize and damage cancer cells.
How does targeted therapy work?
Many targeted therapy medicines work against breast cancer by affecting specific proteins that help cancer cells grow.
Cells usually divide and grow when certain proteins bind to other proteins on the surface of a cell. Some targeted therapies block this binding process, which can slow the rapid growth of cancer cells.
Other targeted therapies are combined with chemotherapy in one medicine to create what you can think of as a “smart bomb” medicine. The targeted therapy brings the chemotherapy medicine to the specific proteins on and in cancer cells and then the chemotherapy destroys them. Doctors call these types of targeted therapies antibody-drug conjugates.
When is targeted therapy used for breast cancer?
Targeted therapy can be used to treat breast cancer that:
is metastatic, especially metastatic disease that has grown during treatment with other medicines
is metastatic with a PIK3CA, AKT1, or PTEN mutation
Pregnant women should not get targeted therapies. The little research that has been done suggests that targeted therapies are not safe during pregnancy. Learn more about breast cancer treatments that can be safely given if you’re pregnant.
Targeted therapy vs. chemotherapy
Both targeted therapy and chemotherapy are systemic treatments, meaning they travel throughout the body through the bloodstream.
Chemotherapy medicines kill fast-growing cells, like cancer cells. But chemotherapy medicines can affect both cancer cells and healthy cells — especially cells that also grow quickly, such as cells in your mouth, intestines, and hair follicles.
Targeted therapy medicines target specific proteins in cancer cells, so are generally less likely than chemotherapy to harm healthy cells.
Some targeted therapy medicines may be given along with chemotherapy. For example, some anti-HER2 medicines may be given before or after a chemotherapy infusion.
Targeted therapy medicines for breast cancer
Some targeted therapy medicines are given as infusions into a vein through an IV or a port. Others are pills or capsules that you swallow. Two are given as injections into the thigh.
Afinitor (chemical name: everolimus) treats advanced-stage, hormone receptor-positive, HER2-negative breast cancer.
Avastin (chemical name: bevacizumab) stops the growth of blood vessels that nourish cancer cells.
Dato-DXd (chemical name: datopotamab deruxtecan-dlnk; brand name: Datroway) is an antibody-drug conjugate that treats certain advanced-stage hormone receptor-positive, HER2-negative breast cancers that have grown during previous treatments.
Enhertu (chemical name: fam-trastuzumab-deruxtecan-nxki) is an antibody-drug conjugate that treats certain types of HER2-positive breast cancer, as well as breast cancer that has a small amount of HER2 proteins on the surface of its cells, which used to be classified as HER2-negative.
Herceptin (chemical name: trastuzumab) treats all stages of HER2-positive breast cancer.
Ibrance (chemical name: palbociclib) is a CDK4/6 inhibitor that treats metastatic, hormone receptor-positive, HER2-negative breast cancer.
Inavolisib (brand name: Itovebi) is a pill used in combination with Faslodex and Ibrance to treat certain advanced-stage breast cancers that have a PIK3CA mutation.
Kadcyla (chemical name: T-DM1 or ado-trastuzumab emtansine) is an antibody-drug conjugate that treats all stages of HER2-positive breast cancer.
Kisqali (chemical name: ribociclib) is a CDK4/6 inhibitor that treats metastatic, hormone receptor-positive, HER2-negative breast cancer.
Lynparza (chemical name: olaparib) treats HER2-negative breast cancers in people with a BRCA1 or BRCA2 mutation.
Margenza (chemical name: margetuximab-cmkb) treats metastatic HER2-positive breast cancer.
Nerlynx (chemical name: neratinib) treats all stages of HER2-positive breast cancer.
Perjeta (chemical name: pertuzumab) treats all stages of HER2-positive breast cancer.
Phesgo (chemical name: pertuzumab, trastuzumab, and hyaluronidase-zzxf) is a combination of Herceptin and Perjeta that is given as an injection in the thigh. It’s used to treat all stages of HER2-positive breast cancer.
Piqray (chemical name: alpelisib) treats metastatic, hormone receptor-positive, HER2-negative breast cancer with a PIK3CA mutation.
Talzenna (chemical name: talazoparib) treats HER2-negative breast cancers in people with a BRCA1 or BRCA2 mutation.
Trodelvy (chemical name: sacituzumab govitecan-hziy) is an antibody-drug conjugate that treats metastatic, hormone receptor-positive, HER2-negative breast cancer that has grown during previous treatment.
Truqap (chemical name: capivasertib) treats metastatic, hormone receptor-positive, HER2-negative breast cancer with a PIK3CA, AKT1, or PTEN mutation.
Tukysa (chemical name: tucatinib) treats metastatic, HER2-positive breast cancer that has grown during previous treatment.
Tykerb (chemical name: lapatinib) treats metastatic, HER2-positive breast cancer.
Verzenio (chemical name: abemaciclib) is a CDK4/6 inhibitor that treats all stages of hormone receptor-positive, HER2-negative breast cancer.
Paying for targeted therapy
If your doctor prescribes a targeted therapy medicine and you have difficulties getting it covered by insurance or don’t have insurance, the company that makes the medicine may be able to help. Use the links above to learn about assistance programs for each medicine.
Research News on targeted therapies
Researchers are always looking for new breast cancer treatments, including new targeted therapies. Read summaries of the most recent studies on targeted therapy.
— Last updated on June 10, 2025 at 4:15 PM
