HER2 Targeting Anticancer Drugs Approved by the FDA^a

Brand Name (Generic Drug Name)

Indications

Enhertu (fam-trastuzumab deruxtecan-nxki)¹

Treatment of adults with HER2-positive, unresectable or metastatic breast cancer who received a prior anti-HER2-based regimen in the metastatic setting or in the neoadjuvant or adjuvant setting and had disease recurrence during or within 6 months of completing therapy

Treatment of adults with HER2-low, unresectable or metastatic breast cancer who received a prior chemotherapy in the metastatic setting or had disease recurrence during or within 6 months of completing adjuvant chemotherapy

Treatment of adults with HER2-positive, unresectable or metastatic NSCLC who have received prior systemic therapy

Treatment of adults with HER2-positive, locally advanced or metastatic gastric or GEJ adenocarcinoma who received a prior trastuzumab-based regimen

Herceptin (trastuzumab)²

Adjuvant treatment of adults with HER2-overexpressing, node-positive or node-negative breast cancer as part of a regimen consisting of doxorubicin, cyclophosphamide, and either paclitaxel or docetaxel; as part of a treatment regimen with docetaxel and carboplatin; or as a single agent following multi-modality anthracycline-based therapy, based on an FDA-approved companion diagnostic for trastuzumab

In combination with paclitaxel for the treatment of adults with HER2-overexpressing metastatic breast cancer in the first-line or as a single agent for HER2-overexpressing breast cancer in patients who received ≥1 chemotherapy regimens for metastatic disease

Herceptin Hylecta (trastuzumab + hyaluronidase-oysk)³

Adjuvant treatment of adults with HER2 overexpressing, node-positive or node-negative breast cancer as part of a regimen comprising doxorubicin, cyclophosphamide, and either paclitaxel or docetaxel; as part of a regimen with docetaxel and carboplatin; or as a single agent following multi-modality anthracycline-based therapy

In combination with paclitaxel for the first-line treatment of adults with HER2-overexpressing, metastatic breast cancer, or as a single agent for the treatment of adults with HER2-overexpressing breast cancer who received ≥1 chemotherapy regimens for metastatic disease

Herzuma (trastuzumab-pkrb)⁴

Adjuvant treatment of HER2-overexpressing, node-positive or node-negative breast cancer as part of a regimen comprising doxorubicin, cyclophosphamide, and either paclitaxel or docetaxel; as part of a regimen with docetaxel and carboplatin; or as a single agent following multi-modality anthracycline-based therapy, based on an FDA-approved companion diagnostic for trastuzumab

In combination with paclitaxel for the first-line treatment of HER2-overexpressing, metastatic breast cancer or as a single-agent for the treatment of HER2-overexpressing breast cancer in patients who received ≥1 chemotherapy regimens for metastatic disease, based on an FDA-approved companion diagnostic trastuzumab

In combination with cisplatin and capecitabine or 5-fluorouracil for the treatment of patients with HER2 overexpressing, metastatic gastric, or GEJ adenocarcinoma who have not previously received treatment for metastatic disease, based on an FDA-approved companion diagnostic for trastuzumab

Kadcyla (ado-trastuzumab emtansine)⁵

Treatment of patients with HER2-positive, metastatic breast cancer who previously received trastuzumab and a taxane, separately or in combination

Adjuvant treatment of patients with HER2-positive, early breast cancer who have residual invasive disease after neoadjuvant taxane and trastuzumab-based therapy

Margenza (margetuximab-cmkb)⁶

In combination with chemotherapy for the treatment of adult patients with metastatic HER2-positive breast cancer who have received ≥2 prior anti-HER2 regimens, at least 1 of which was for metastatic disease

Nerlynx (neratinib)⁷

Extended adjuvant treatment of adults with early-stage, HER2-positive breast cancer, after adjuvant trastuzumab-based therapy

In combination with capecitabine for the treatment of adults with HER2-positive, advanced or metastatic breast cancer who received ≥2 prior anti-HER2 based regimens in the metastatic setting

Ogivri (trastuzumab-dkst)⁸

Treatment of HER2-overexpressing breast cancer

Treatment of HER2-overexpressing, metastatic gastric or gastroesophageal junction adenocarcinoma

Ontruzant (trastuzumab-dttb)⁹

Treatment of HER2-overexpressing breast cancer, based on an FDA-approved companion diagnostic for trastuzumab

Treatment of HER2-overexpressing, metastatic gastric or gastroesophageal junction adenocarcinoma, based on an FDA-approved companion diagnostic for trastuzumab

Perjeta (pertuzumab)¹⁰

In combination with trastuzumab and docetaxel for the treatment of patients with HER2-positive, metastatic breast cancer who have not received prior anti-HER2 therapy or chemotherapy for metastatic disease

In combination with trastuzumab and chemotherapy as neoadjuvant treatment for patients with HER2-positive, locally advanced, inflammatory, or early-stage breast cancer as part of a complete regimen for early breast cancer or as adjuvant treatment for patients with HER2-positive, early breast cancer at high risk for recurrence

Phesgo (pertuzumab, trastuzumab, + hyaluronidase-zzxf)¹¹

In combination with chemotherapy as neoadjuvant treatment for patients with HER2-positive, locally advanced, inflammatory, or early-stage breast cancer as part of a complete regimen for early breast cancer or as adjuvant treatment for patients with HER2-positive, early breast cancer at high risk for recurrence

In combination with docetaxel for the treatment of patients with HER2-positive, metastatic breast cancer who have not received prior anti-HER2 therapy or chemotherapy for metastatic disease

Trazimera (trastuzumab-qyyp)¹²

Treatment of HER2-overexpressing breast cancer, based on an FDA-approved companion diagnostic for trastuzumab

Treatment of HER2-overexpressing metastatic gastric or gastroesophageal junction adenocarcinoma, based on an FDA-approved companion diagnostic for trastuzumab

Tukysa (tucatinib)¹³

In combination with trastuzumab and capecitabine for the treatment of adults with advanced, unresectable or metastatic HER2-positive breast cancer, including patients with brain metastases, who received ≥1 HER2-targeted regimens in the metastatic setting

Tykerb (lapatinib)¹⁴

In combination with capecitabine for the treatment of patients with advanced or metastatic breast cancer that overexpresses HER2 who received prior therapy, including an anthracycline, a taxane, and trastuzumab

In combination with letrozole for the treatment of postmenopausal women with HR-positive, metastatic breast cancer that overexpresses HER2 for whom hormonal therapy is indicated

Vizimpro (dacomitinib)¹⁵

First-line treatment of patients with metastatic NSCLC with EGFR exon 19 deletion or exon 21 L858R substitution mutations as detected by an FDA-approved test

HER2 Targeting Anticancer Drugs in the Pipeline^b

Brand Name (Generic Drug Name)

Potential Indications

Enhertu (fam-trastuzumab deruxtecan-nxki)¹⁶

Being evaluated for the treatment of patients with HER2-positive breast cancer; HER2-low breast cancer; HER2-positive, unresectable and/or metastatic breast cancer previously treated with standard of care HER2 therapies, including ado-trastuzumab emtansine; HER2-positive, unresectable and/or metastatic breast cancer previously treated with trastuzumab and taxane; HER2-low, unresectable and/or metastatic breast cancer; HER2-positive, high-risk breast cancer; HER2-low, HR-positive breast cancer; HER2-overexpressing, advanced gastric or gastroesophageal junction adenocarcinoma that progressed with 2 prior treatment regimens; HER2-positive gastric cancer; HER2-positive or HER2-over-expressing, unresectable and/or metastatic NSCLC; HER2-positive NSCLC; HER2-positive solid tumors

Faslodex (fulvestrant)

GDC-0077 (inavolisib)¹⁷

Being evaluated for the neoadjuvant endocrine treatment of patients with early-stage, HER2-positive, HR-positive, PIK3CA mutant breast cancer

OP-1250¹⁸

Being evaluated for the treatment of patients with ER-positive/HER2-positive, metastatic breast cancer with CNS metastases

Perjeta (pertuzumab)¹⁹

Being evaluated in combination with trastuzumab emtansine for the treatment of patients with early, HER2-positive breast cancer; in combination with atezolizumab for the treatment of patients with early, metastatic, HER2-positive breast cancer

RG6171 (giredestrant)²⁰

Being evaluated in combination with Phesgo (pertuzumab, trastuzumab, + hyaluronidase-zzxf) for the first-line treatment of patients with ER-positive, HER2-positive breast cancer

RG6194 (runimotamab)¹⁷

Being evaluated for the treatment of patients with metastatic, HER2-expressing cancers

SAR446309 (formerly known as AMX-818)²¹

Being evaluated for the treatment of patients with solid tumors

SHR6390 (dalpiciclib)²²

Being evaluated for the treatment of patients with HER2-positive gastric cancer

Kadcyla (ado-trastuzumab emtansine)¹⁷

Being evaluated for the first-line treatment of patients with HER2-positive, metastatic breast cancer; in combination with pertuzumab for the treatment of patients with early, HER2-positive breast cancer; in combination with atezolizumab for the treatment of patients with early, HER2-positive breast cancer; in combination with atezolizumab or placebo for the treatment of patients with HER2- and PD-L1–positive locally advanced or metastatic breast cancer previously treated with trastuzumab- (± pertuzumab) and taxane-based therapy; for the treatment of high-risk patients with HER2-positive early breast cancer; for the third-line treatment of patients with HER2-positive, metastatic breast cancer

CNS, central nervous system; EGFR, epidermal growth factor receptor; ER, estrogen receptor; ET, endocrine therapy; GEJ, gastroesophageal junction; HR, hormone receptor; NSCLC, non-small-cell lung cancer.

^aAdapted from prescribing information.^1-15

^bAdapted from manufacturer websites.^16-22