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Targeted therapy pills: how these drugs work
Targeted therapy pills block specific proteins or gene changes that help a cancer grow. Many of them only work if your tumor has the matching change, which is why biomarker testing is so important, especially in lung cancer. Because they aim at a target, their side effects are usually different from chemo. Rash, diarrhea, and liver or blood count changes are common, while severe hair loss is less common. Most are taken at home every day for as long as they keep working. That makes taking them on time, watching for side effects, and keeping up with blood tests a big part of daily life. Some interact with other medicines or with grapefruit, so check with your pharmacist before starting anything new.
ℹ️ General information to help you and your loved ones talk with your care team, not medical advice. Read our disclaimer.
On this page: EGFR inhibitors · ALK inhibitors · ROS1 and NTRK inhibitors · TRK inhibitors · MET inhibitors · RET inhibitors · KRAS G12C inhibitors · BRAF inhibitors · MEK inhibitors · CDK4/6 inhibitors · PI3K inhibitors · AKT inhibitors · HER2 pills · PARP inhibitors · PARP inhibitor plus hormone therapy · VEGFR inhibitors · Multikinase inhibitors
EGFR inhibitors
These pills block EGFR mutations in non-small cell lung cancer. Tagrisso (osimertinib) is the most used today. Older ones include Tarceva (erlotinib), Iressa (gefitinib), Gilotrif (afatinib), and Vizimpro (dacomitinib), and Lazcluze (lazertinib) is used with Rybrevant (amivantamab). Rash, dry skin, nail-fold soreness, and diarrhea are typical.
ALK inhibitors
For ALK-positive lung cancer: Alecensa (alectinib), Alunbrig (brigatinib), and Lorbrena (lorlatinib). They reach the brain well, which matters because ALK cancer often spreads there. Lorbrena can raise cholesterol and affect mood or thinking, and Alunbrig can cause breathing problems in the first week.
ROS1 and NTRK inhibitors
Rozlytrek (entrectinib) and Augtyro (repotrectinib) block ROS1 fusions in lung cancer and NTRK fusions in many solid tumors. Dizziness, taste changes, and weight gain are common.
TRK inhibitors
Vitrakvi (larotrectinib) is for NTRK gene fusions in any solid tumor. These fusions are rare, but the drug often works well when one is found.
MET inhibitors
Tabrecta (capmatinib) and Tepmetko (tepotinib) treat lung cancer with MET exon 14 skipping. Swelling in the legs and hands (edema) is the most common side effect.
RET inhibitors
Retevmo (selpercatinib) and Gavreto (pralsetinib) block RET fusions in lung cancer and other tumors. High blood pressure and liver test changes are watched.
KRAS G12C inhibitors
Lumakras (sotorasib) and Krazati (adagrasib) block the KRAS G12C mutation in lung cancer and, combined with an EGFR antibody, in colorectal cancer. Diarrhea, nausea, and liver changes are common.
BRAF inhibitors
Tafinlar (dabrafenib) and Braftovi (encorafenib) block BRAF V600E. They're always paired with a partner drug: a MEK inhibitor in lung cancer, or an EGFR antibody in colorectal cancer.
MEK inhibitors
Mekinist (trametinib) blocks MEK, the next step after BRAF in the same pathway, and is taken with Tafinlar. Fever is a well-known side effect of the pair.
CDK4/6 inhibitors
Ibrance (palbociclib), Kisqali (ribociclib), and Verzenio (abemaciclib) slow cell division in HR-positive breast cancer and are taken with hormone therapy. Low white blood cells are common. Verzenio is known for diarrhea, and Kisqali for heart rhythm and liver checks.
PI3K inhibitors
Piqray (alpelisib) and Itovebi (inavolisib) target PIK3CA-mutated, HR-positive breast cancer. High blood sugar is the key side effect, so blood sugar is checked often.
AKT inhibitors
Truqap (capivasertib) blocks AKT in HR-positive breast cancer with PIK3CA, AKT1, or PTEN changes, together with Faslodex (fulvestrant). Diarrhea, rash, and high blood sugar can occur.
HER2 pills
Nerlynx (neratinib) and Tukysa (tucatinib) block HER2 from inside the cell in HER2-positive breast cancer, and Tukysa also in colorectal cancer. Diarrhea is the main side effect, especially with Nerlynx.
PARP inhibitors
Lynparza (olaparib), Zejula (niraparib), Rubraca (rucaparib), and Talzenna (talazoparib) stop cancer cells with BRCA or other DNA-repair problems from fixing their DNA. They're used in ovarian, breast, and prostate cancer. Tiredness, nausea, and anemia (low red blood cells) are common.
PARP inhibitor plus hormone therapy
Akeega combines niraparib and abiraterone in one tablet for BRCA-mutated metastatic prostate cancer. It's taken with prednisone.
VEGFR inhibitors
Fruzaqla (fruquintinib) blocks the signals tumors use to grow new blood vessels, for colorectal cancer after earlier treatments. High blood pressure and hand-foot skin reactions are common.
Multikinase inhibitors
Stivarga (regorafenib) blocks several growth and blood-vessel signals at once, for colorectal cancer after earlier treatments. Hand-foot skin reaction and tiredness are common, and liver tests are checked.
Taking pills at home safely
Keep a daily log, use a pill box or phone alarm, and don't stop or change your dose without talking to your team. If side effects build up, a dose reduction is common and often keeps the drug working while you feel better. Ask about copay help early, since many of these pills are expensive. Our cost help guide can help.
Side effect guides that may help
- Dermatitis (skin rash and skin changes)
- Diarrhea (loose, watery stools)
- Fatigue (extreme tiredness)
- Mucositis (mouth sores)
❓ Questions you and your loved ones can ask
- What is the goal of this treatment for me?
- How will we know if it's working?
- Which side effects should I call about right away, and what number do I call after hours?
- Which medicines, vitamins or supplements should I avoid?
- Will this affect my ability to work, drive, or care for my family?
- What will this cost me, and who can help me with coverage?
Written by the CSE Team from FDA labels and leading cancer centers. Not medical advice. · Last updated: October 15, 2026 · How we write
Sources
Last updated: October 15, 2026. We summarize these sources in our own words.