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Targeted Therapy for Treating Cancer
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for Cancer Treatment

Targeted therapies are designed to attack or kill cancer cells, while sparing normal cells as much as possible. These therapies are often designed to attach to abnormal proteins, receptors or genes that are found in high quantities in cancer cells or the surrounding tissue.  

This section covers the following topics. 

How are targeted therapies selected?

Some, but not all targeted therapies work best against cancer cells with certain markers or mutations. Two important types of tests can help guide selection of these targeted therapies.

  • testing involves looking at tumor, blood or other other tissue samples for abnormal markers that might indicate the cancer is likely to respond to a particular . You can learn more about testing for selecting targeted therapies in our Biomarkers sections.
  • Genetic testing for inherited mutations can also help guide treatment with targeted therapies. PARP inhibitors, for example, are a type of that are most effective for treating cancer in people with a or mutation. 

Each  drug has different indications. Like all cancer treatments, targeted therapies can have side effects. Visit our section on Side Effects for more information.

Image of how targeted therapy works

PARP inhibitors

PARP inhibitors work by blocking a protein used to repair damaged . They were initially developed to treat cancers in people with an inherited or mutation. Since then, research and additional approvals have expanded use of PARP inhibitors to more people and situations. There are five PARP inhibitors that have received  approval for treating different types of cancers. 

Indications vary by:

  • type and  of cancer: PARP inhibitors have been approved to treat breast, ovarian, pancreatic and cancers.
  • presence of a mutation or biomarker: PARP inhibitors have been approved in different settings for:  
    • people with certain inherited mutations.
    • people with certain acquired mutations.
    • people with certain tumor biomarkers.
    • women with certain types of ovarian cancer, regardless of the presence of an or .
  • number of and response to prior treatments:  have been approved in different settings for:
    • platinum-sensitive or partially platinum-sensitive ovarian cancer. 
    • castration-resistent cancer (mCRPC).
    • after chemotherapy. 
    • to treat progression or recurrence after a specific number of prior treatments. 

Clinical trials studying PARP inhibitors in new settings or combinations are enrolling patients. As research continues, these approvals may expand to include treatment for additional cancers, earlier stages of cancer, people with other inherited mutations, and based on different tumor biomarkers.

Table of PARP inhibitors

Open Table
Table of PARP Inhibitors: This table lists different PARP inhibitors and their indications.

Drug

Cancer Type

Use

Lynparza ()

Breast cancer

Early breast cancer at high risk for recurrence

Given for one year as after completion of or chemotherapy and local treatment (surgery and, or radiation).

or inherited mutation ()

Lynparza ()

Breast cancer

For treatment of patients who have previously received chemotherapy, or hormone therapy for patients with hormone receptor disease.

or inherited mutation and

()

Breast cancer

For treatment of breast cancer.

or mutation and

Lynparza ()

Ovarian cancer

3 or 4

maintenance therapy for people who had a complete or partial response to platinum chemotherapy.

  • Inherited () mutation in or
  • Tumor (somatic) mutation in or

Lynparza ()

Ovarian cancer

3 or 4

Combined with Avastin (bevacuzimab) for people who had a complete or partial response to platinum chemotherapy.

  • in or , or
  • HRD-positive ( Deficiency-positive)

Lynparza
()


()


()

Ovarian cancer

3 or 4

Second-line or later for people who had a complete or partial response to platinum chemotherapy.

No needed

()

Ovarian cancer

3 or 4

For people who had a complete or partial response to platinum chemotherapy.

No required

Lynparza ()

Pancreatic cancer

For people whose disease has not progressed on at least 16 weeks of platinum-based chemotherapy.

in or

Akeega ( and acetate)

cancer

castration-resistant cancer (mCRPC)

In combination with prednisone for or later treatment of mCRPC.

Inherited or tumor mutation in or based on FoundationOne tumor test

Lynparza ()

cancer

castration-resistant cancer (mCRPC)

Combined with Zytiga and prednisone or prednisolone for or later treatment of mCRPC.

  • in or found through genetic testing, or
  • Tumor or mutation found through tumor testing or

Lynparza ()

cancer

castration-resistant cancer (mCRPC)

For treatment of mCRPC which has progressed following treatment with Xtandi () or Zytiga ().

  • in or , or
  • Tumor mutation in one of the following genes: , , , , , CDK12, , FANCL, , RAD51B, , , RAD54

()

cancer

castration-resistant cancer (mCRPC)

For treatment of mCRPC which has been treated with androgen receptor-directed therapy and a taxane-based chemotherapy.

  • in or found through genetic testing, or
  • Tumor or mutation found through tumor testing or

()

cancer

castration-resistant cancer (mCRPC)

In combination with for mCRPC which has not yet been treated in the castration-resistant setting.

Inherited or tumor mutation in one of the following genes: , , , ATR, CDK12, , FANCA, , MRE11A, , , or

Other targeted therapies

There is a growing list of FDA-approved targeted therapies for cancer treatment. Most are classified by the abnormal target that they are designed to bind to and attack. Many of these new therapies are approved for use in all types of cancers () as long as the cancer contains the right marker or target. Drugs that are approved across cancer types are sometimes called pan-tumor or tumor-agnostic therapies. 

Some drugs are classified as both immunotherapies and targeted therapies because they use antibodies to target abnormal proteins or receptors that are found in high quantities in cancer cells or the surrounding tissue. Antibody drug conjugates (ADCs) are drugs that combine two different types of molecules.  A chemotherapy drug is linked to an antibody that delivers the chemotherapy directly to the cancer cells. 

The table below lists some common targeted therapies used in cancer treatment. Clincal trials are studying new agents for treating cancer. 

Table of targeted therapies

Open Table
Table of Targeted Therapies: This table lists commonly used targeted therapies and their indications.

Drug

Cancer Type

Use

Type of Agent

Afinitor
(everolimus)

Breast cancer

or advanced

Combined with exemestane for postmenopausal women with advanced breast cancer which progressed with letrozole or anastrozole.

,

MTOR inhibitor

Afinitor
(everolimus)

Pancreatic neuro-endocrine tumors (PNET)

Progressive PNETs

Used to treat PNETs that have progressed on other treatments.

No needed

MTOR inhibitor

Avastin
(bevacizumab)

Ovarian, or primary peritoneal cancer

2-4

Combined with Lynparza () for maintenance therapy for platinum-sensitive cancer.

()
testing

VEGF inhibitor

Avastin
(bevacizumab)

Ovarian, or primary peritoneal cancer

3-4

Combined with chemotherapy, followed by Avastin as a single agent following initial surgical resection.

No needed

VEGF inhibitor

Avastin
(bevacizumab)

Ovarian, or primary peritoneal cancer

Recurrent

Combined with chemotherapy for treating platinum-resistant, recurrent disease in people who received no more than 2 prior chemotherapy regimens.

No needed

VEGF inhibitor

Avastin
(bevacizumab)

Ovarian, or primary peritoneal cancer

Recurrent

Combined with chemotherapy, followed by Avastin as a single agent, for platinum-sensitive recurrent disease.

No needed

VEGF inhibitor

Avastin
(bevacizumab)

Colorectal cancer

Combined with intravenous 5-fluorouracil-based chemotherapy for first-, or second-line treatment.

No needed

VEGF inhibitor

Avastin
(bevacizumab)

Colorectal cancer

Combined with chemotherapy for second-line treatment in patients who have progressed on a Avastin-containing regimen.

No needed

VEGF inhibitor

Braftovi
(encorafenib)

Colorectal cancer

Combined with cetuximab, for the treatment of adult patients with colorectal cancer.

BRAF V600E tumor mutation

BRAF inhibitor

Braftovi
(encorafenib)

Melanoma

Combined with Mektovi (binimetinib), for the treatment of patients with unresectable or melanoma.

BRAF V600E or V600K tumor mutation

BRAF inhibitor

Cotellic
(cobimetinib)

Melanoma

Combined with Zelboraf (vemurafenib) for the treatment of patients with unresectable or melanoma.

BRAF V600E or V600K tumor mutation

BRAF inhibitor

Cyramza
(ramucirumab)

Colorectal cancer

Combined with FOLFIRI chemotherapy, for treatment after disease progression on, or after prior therapy with bevacizumab, oxaliplatin, and a fluoropyrimidine.

No required

VEGF inhibitor

Datroway (datopotamab deruxtecan-dlnk)

Breast cancer

Treatment for cancers that have progressed after hormone therapy and chemotherapy.

Hormone receptor position (),

Antibody-drug conjugate (chemotherapy attached to antibody targeting TROP-2)

ELAHERE (mirvetuximab soravtansine-gynx)

Ovarian cancer

3-4

Used as second-line or later treatment of platinum-resistant or platinum-sensitive recurrent ovarian cancer.

Positive for FRα (folate receptor alpha)

Antibody-drug conjugate (chemotherapy attached to antibody targeting FR-α receptor)

Enhertu (fam-trastuzumab-deruxtecan-nxki)

Breast cancer

Treatment for people who have received a prior anti-HER2-based regimen either:

  • in the setting.
  • in the or setting and developed a recurrence during or within six months of completing treatment.

overexpression ()

Antibody-drug conjugate

Enhertu (fam-trastuzumab-deruxtecan-nxki)

Breast cancer

As treatment for people who have tumors that are HER2-low, received chemotherapy in the setting and whose cancer no longer responds to hormonal therapy.

and HER2-low

Antibody-drug conjugate

Enhertu (fam-trastuzumab-deruxtecan-nxki)

Breast cancer

As treatment for people with , HER2-low or ultralow that came back or got worse after one or more hormone therapies in the setting.

and HER2-low or HER2-ultra low

Antibody-drug conjugate

Enhertu (fam-trastuzumab-deruxtecan-nxki)

(pan tumor)

or unresectable

For adult patients with unresectable or , solid tumors (including colorectal cancer) who have received prior systemic treatment and have no alternative treatment options.

overexpression ()

Antibody-drug conjugate

Erbitux
(cetuximab)

Colorectal cancer

Combined with FOLFIRI for treatment, or combined with irinotecan for cancers that no longer respond to irinotecan-based chemotherapy or as a single agent in patients who have progressed after oxaliplatin- and irinotecan-based chemotherapy.

EGFR positive and KRAS mutation negative

EGFR inhibitor

Fruzaqla
(fruquintinib)

Colorectal cancer

Used as a single agent when cancer has progressed after treatment with chemotherapy and .

No required

VEGF inhibitor

Herceptin
(trastuzumab)

Breast cancer

Early

The treatment of breast cancer.

overexpression ()

Antibody targeting receptors

Herceptin (trastuzumab) and Tukysa (tucatinib) combination

Colorectal cancer

or unresectable

For people who progressed after chemotherapy.

overexpression ()

Antibody targeting receptors and a kinase inhibitor that targets receptors

Ibrance
(palbociclib)

Breast cancer

Combined with an aromatase inhibitor as treatment of advanced cancer as initial hormone therapy in postmenopausal women or in men.

and

known as a kinase inhibitor that blocks the CDK4/6 pathway

Ibrance
(palbociclib)

Breast cancer

Combined with Faslodex (fulvestrant) as treatment in postmenopausal women or in men whose disease progressed following endocrine therapy.

and

known as a kinase inhibitor that blocks the CDK4/6 pathway

Kadcyla
(trastuzumab emtansine)

Breast cancer

Early

therapy for people with early breast cancer who still have disease after taxane and treatment with Herceptin

overexpression ()

Antibody targeting receptors

Kadcyla
(trastuzumab emtansine)

Breast cancer

For treatment in people whose cancer got worse after receiving Herceptin and chemotherapy in the following settings:

  • for disease, or
  • as therapy, and experienced disease recurrence during or within 6 months of completing therapy.

overexpression ()

Antibody targeting receptors

Kisqali
(ribociclib)

Breast cancer

Combined with an aromatase inhibitor for the treatment of pre/perimenopausal or postmenopausal women as initial hormone based therapy.

and

known as a kinase inhibitor that blocks the CDK4/6 pathway

Kisqali
(ribociclib)

Breast cancer

Combined with Faslodex (fulvestrant) for the treatment of postmenopausal women, as initial hormone based therapy.

and

known as a kinase inhibitor that blocks the CDK4/6 pathway

Krazati (adagrasib)

Colorectal cancer

In combination with cetuximab for locally advanced or colorectal cancer (CRC) that has progressed after treatment with chemotherapy.

KRASG12C mutation

against the KRASG12C protein

Lenvima (lenvatinib)

Endometrial cancer

Advanced disease

Combined with pembrolizumab, for the treatment of patients whose cancer has progressed after treatment and who are not candidates for surgery or radiation.

Tumors that are not MSI-H or (or ) - they may be referred to as MSI-Low, MSS, pMMR or MMR-P)

known as a tyrosine kinase inhibitor

Mekinist (trametinib)

Melanoma

Unresectable or

As a single agent and in combination with dabrafenib for the treatment of unresectable or melanoma.

BRAF V600E or V600K tumor mutation

known as a MEK inhibitor

Mekinist (trametinib)

Melanoma

Lymph node positive

Combined with Taflinar (dabrafenib) as treatment of people with melanoma and involvement of lymph node(s), following complete resection.

BRAF V600E or V600K tumor mutation

known as a MEK inhibitor

Mektovi (binimetinib)

Melanoma

Unresectable or

Combined with Braftovi (encorafenib), for the treatment of people with unresectable or melanoma.

BRAF V600E or V600K tumor mutation

known as a MEK inhibitor

Orserdu
(elacestrant)

Breast cancer

Used alone to treat men or postmenopausal women with , breast cancer, which progressed after at least one line of hormone therapy therapy.

, with an ESR1 mutation

Type of targeted hormonal therapy known as SERD (selective receptor degrader or downregulator)

Perjeta (pertuzumab)

Breast cancer

Locally advanced, inflammatory or early

Combined with Herceptin (trastuzumab) and docetaxel as treatment before surgery ().

overexpression ()

Antibody targeting receptors

Phesgo (pertuzumab, trastuzumab combined injection)

Breast cancer

Early

  • Before surgery () treatment for tumors larger than 2 cm or node-positive, or
  • After surgery () treatment for early breast cancer that has a high likelihood of coming back.

overexpression ()

Antibody targeting receptors

Piqray
(alpelisib)

Breast cancer

Combined with Faslodex (fulvestrant) as treatment in men or post-menopausal women who progressed on or after treatment with hormone therapy.

, and positive for a PIK3CA tumor mutation

known as a kinase inhibitor that blocks the PIK3 pathway

Pluvicto (lutetium Lu 177 vipivotide tetraxetan)

cancer

castration-resistant cancer (mCRPC)

For treatment of mCRPC which has stopped responding or got worse after treatment with hormonal therapy using an androgen receptor inhibitor and taxane-based chemotherapy.

Imaging with a that looks for cancers with the marker PSMA

Targeted radiation therapy (radioligand therapy)

Retevmo (selpercatinib)

(pan tumor)

or unresectable

Second-line or later treatment for solid tumors for which there are no other treatment options.

RET fusion

Kinase inhibitor

Stivarga (regorafenib)

Colorectal cancer

For treatment of colorectal cancer that has progressed after treatment and for which there are no other treatment options.

No required

known as a multi-kinase inhibitor

Tafinlar
(dabrafenib)

Melanoma

Unresectable or

Combined with Mekinist (trametinib) for the treatment of people with unresectable or melanoma.

BRAF V600E or V600K tumor mutation

known as a BRAF inhibitor

Tafinlar
(dabrafenib)

Melanoma

Lymph node positive

Combined with Mekinist (trametinib) as treatment of people with melanoma and involvement of lymph node(s), following complete resection.

BRAF V600E or V600K tumor mutation

known as a BRAF inhibitor

Trodelvy (sacituzumab govitecan-hziy)

Breast cancer

For breast cancer that progressed, recurred or did not respond to at least two previous lines of treatment.

Triple-negative (, )

Antibody-drug conjugate (chemotherapy attached to antibody found in )

Truqap
(capivasertib)

Breast cancer

Combined with fulvestrant as treatment for , advanced or breast cancer which recurred or got worse after standard hormone therapy.

, PIK3 or AKT1 mutation in the tumor

known as a kinase inhibitor that blocks the AKT pathway

Tukysa (tucatinib)

Breast cancer

or unresectable

In combination with Herceptin (trastuzumab) to treat cancer which has progressed after at least one prior treatment with an anti-HER2 treatment in the setting.

overexpression ()

known as a kinase inhibitor that targets receptors

Vectibix
(panitumumab)

Colorectal cancer

Combined with FOLFOX for treatment.

Negative for KRAS and NRAS mutations

that targets a receptor known as EGFR

Vectibix
(panitumumab)

Colorectal cancer

As a single therapy following disease progression after prior treatment with fluoropyrimidine, oxaliplatin, and irinotecan-containing chemotherapy.

Negative for KRAS and NRAS mutations

that targets a receptor known as EGFR

Verzenio (abemaciclib)

Breast cancer

Used alone to treat breast cancer that has progressed after treatment with hormone therapy and chemotherapy in the setting.

and

known as a kinase inhibitor that blocks the CDK4/6 pathway

Verzenio (abemaciclib)

Breast cancer

Combined with Faslodex (fulvestrant) as treatment in women whose disease progressed following endocrine therapy.

and

known as a kinase inhibitor that blocks the CDK4/6 pathway

Vitrakvi (larotrectinib)

(pan tumor)

or unresectable

For treatment in solid tumors for which there are no other treatment options.

NTRK fusion

Kinase inhibitor

Xofigo (Radium 223 dichloride)

cancer

castration-resistant cancer (mCRPC)

For treatment of mCRPC that has spread to the bones but has not to other organs.

No needed

Targeted radiation therapy (radioligand therapy)

Zelboraf (vemurafenib)

Melanoma

Unresectable or

Combined with Tecentriq (atezolizumab) and Cotellic (cobimetinib) in people with melanoma that has the BRAF gene mutation, when the cancer can’t be removed by surgery or has spread to other parts of the body.

BRAF V600E or V600K tumor mutation

known as a BRAF inhibitor

Last updated February 05, 2025