. 2022 Mar 5;23(5):2856. doi: 10.3390/ijms23052856

Table 3.

Breast cancer drugs approved by the US Food and Drug Administration.

Generic Name or Brand Name	Background	Molecular Structure	Stage	Dosage &Strength	Route	References
Trastuzumab (Herceptin)	Trastuzumab is a recombinant IgG1 kappa, humanized monoclonal antibody that selectively binds with high affinity in a cell-based assay (Kd = 5 nM) to the extracellular domain of the human epidermal growth factor receptor protein (HER2).	C₆₄₇₀H₁₀₀₁₂N₁₇₂₆O₂₀₁₃S₄₂	HER2+	Powder, for solution (440 mg/ vial)	Iv	[13,14]
				Injection, powder, for solution (150 mg, 150 mg/7.4 mL).	Iv
				Injection, solution (600mg)	Sc
Pertuzumab (Perjeta)	Pertuzumab is an antineoplastic agent used in the treatment of HER2-positive metastatic breast cancer in combination with other antineoplastic agents.	C₁₇H₂₇NO₂	Metastatic HER2+ in patients who have not been treated with hormone therapy or chemotherapy.	Injection, solution, concentrate (420 mg)	Iv	[15]
			As neoadjuvant therapy in patients with locally advanced, inflammatory, or early-stage cancer; as adjuvant therapy in patients with early-stage cancer who have a high recurrence risk	Pertuzumab (420 mg/14 mL) + Trastuzumab (440 mg/vial),Powder, for solution; Solution.	Iv
				Pertuzumab (1200 mg) + Trastuzumab (600 mg), Injection, Solution.	Sc
				Pertuzumab (1200 mg/15 mL) + Hyaluronidase (human recombinant) (30,000 U/15 mL) + Trastuzumab (600 mg/15 mL), Injection, Solution.	Sc
Ado-Trastuzumab Emtansine (Kadcyla)	Ado-Trastuzumab emtansine, is a first-in-class HER2 antibody drug conjugate (ADC) composed of Genentech’s trastuzumab antibody and ImmunoGen’s cell-killing chemical, DM1.	C₆₄₄₈H₉₉₄₈N₁₇₂₀O₂₀₁₂S₄₄•(C₄₇H₆₂C_lN₄O₁₃S)n	Used in patients with HER2-positive metastatic breast cancer who have previously received taxane and/or trastuzumab for metastatic cancer or who had a recurrence of their cancer within six months after adjuvant therapy.	Injection, powder, lyophilized, for solution (20 mg/1 mL, 100 mg)	Iv	[16,17,18]
Ado-Trastuzumab Emtansine (Kadcyla)		C₆₄₄₈H₉₉₄₈N₁₇₂₀O₂₀₁₂S₄₄•(C₄₇H₆₂C_lN₄O₁₃S)n		Powder, for solution (160 mg/vial).	Iv	[16,17,18]
Abemaciclib (Verzenio)	Abemaciclib is an antitumor agent and dual inhibitor of cyclin-dependent kinases 4 (CDK4) and 6 (CDK6) that are involved in the cell cycle and promotion of cancer cell growth in case of unregulated activity.	C₂₇H₃₂F₂N₈	As Monotherapy: Advanced or metastatic HR+ and HER2−	Starting dose: - Combination therapy: 150 mg 2 times a day - Monotherapy: 200 mg orally 2 times a day - First dose reduction: - Combination therapy: 100 mg tablet 2 times a day - Monotherapy: 150 mg tablet orally 2 times a day - Second dose reduction: - Combination therapy: 50 mg tablet 2 times a day - Monotherapy: 100 mg tablet 2 times a day - Third dose reduction: - Combination Therapy: N/A - Monotherapy: 50 mg tablet 2 times a day	Oral	[18,19]
			In combination with an aromatase inhibitor: Initial endocrine-based therapy for postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer
			In combination with fulvestrant: For women with hormone receptor (HR)-positive, (HER2)-negative advanced or metastatic breast cancer with disease progression following endocrine therapy
Cyclophosphamide (Cytoxan, Endoxan, Cycloblastin, Neosar, Revimmune)	Precursor of the alkylating nitrogen mustard anticancer and immunosuppressive drug aldophosphamide, which must be activated in the liver to create the active aldophosphamide	C₇H₁₅Cl₂N₂O₂P	Advanced or metastatic	Injection, powder, for solution (2 g/100 mL)	Iv; Oral	[19,20]
				Tablet (25 mg/L)	Oral
				Capsule (25 mg/L)	Oral
Docetaxel (Taxotere)	Docetaxel is a well-known anti-mitotic chemotherapy drug that is mostly used to treat breast, ovarian, and non-small cell lung cancer. Docetaxel binds to tubulin reversibly and with a high affinity in a 1:1 stoichiometric ratio.	C₄₃H₅₃NO₁₄	Metastatic cancer that has not gotten better with other chemotherapy or node positive cancer removed by surgery	Injection (10 mg/1 mL, 80 mg/4 mL, 160 mg/8 mL)	Iv	[19,21]
Docetaxel (Taxotere)		C₄₃H₅₃NO₁₄		Injection, solution, concentrate(20 mg/1 mL)	Iv	[19,21]
Exemestane (Aromasin)	Exemestane is an oral steroidal aromatase inhibitor used in the adjuvant treatment of hormonally-responsive breast cancer in postmenopausal women. It irreversibly binds to the active site of the enzyme resulting in permanent inhibition.	C₂₀H₂₄O₂	Early stage, advanced or ER+.	Tablet (25 mg)	Oral	[19,22]
Tamoxifen Citrate	Tamoxifen is a selective estrogen receptor modulator used to treat estrogen receptor positive breast cancer, reduce the risk of invasive breast cancer following surgery, or reduce the risk of breast cancer in high risk women.	C₂₆H₂₉NO	Advanced or metastatic ER+	Nolvadex:Tablet(20 mg/L, 10 mg/L)	Oral	[19,23]
				Tamofen:Tablet (10 mg, 20 mg)
				Soltamox:Liquid(20 mg/10 mL or 10 mg/5 mL)
				Tamone:Tablet (10mg)
Anastrazole (Arimidex)	Anastrozole is a non-steroidal aromatase inhibitor (AI) comparable to letrozole that is used to treat postmenopausal women with estrogen-responsive breast cancer.	C₁₇H₁₉N₅	Early-stage, HR+ in women who have already received other treatment; HR+ locally advanced or metastatic breast cancer or hormone receptor unknown; advanced breast cancer that has gotten worse after treatment with tamoxifen citrate	Tablet, film coated (1 mg/mL)	Oral	[19,24]
				Pellet Anastrozole (20 mg/L) + Testosterone (200 mg/L)	Oral
				Pellet, implantable Anastrozole (4 mg/L) + Testosterone (60 mg/L)	Sc
Doxorubicin	Doxorubicin is a cytotoxic anthracycline antibiotic isolated from cultures of Streptomyces peucetius var. caesius.	C₂₇H₂₉NO₁₁	Node-positive cancer removed by surgery	Adriamycin: Solution (2 mg/mL)	Iv; Ives	[19,25]
Doxorubicin		C₂₇H₂₉NO₁₁	Node-positive cancer removed by surgery	Caelyx: Injection, solution, concentrate (2 mg/mL)	Iv	[19,25]
Methotrexate (Rheumatrex, Trexall)	Methotrexate is a folate derivative that inhibits several enzymes responsible for nucleotide synthesis. This inhibition leads to suppression of inflammation as well as prevention of cell division. Because of these effects, methotrexate is often used to treat inflammation caused by arthritis or to control cell division in neoplastic diseases such as breast cancer and non-Hodgkin’s lymphoma	C₂₀H₂₂N₈O₅	Advanced or metastatic	Tablet (2.5 mg/L)	Oral	[19,26]
Methotrexate (Rheumatrex, Trexall)		C₂₀H₂₂N₈O₅	Advanced or metastatic	Solution (25 mg/mL)	Im; Ia; Iv	[19,26]
Vinblastine Sulfate (Velban)	Antitumor alkaloid isolated from Vinca rosea and used to treat breast cancer, testicular cancer, neuroblastoma, Hodgkin’s and non-Hodgkins lymphoma, mycosis fungoides, histiocytosis, and Kaposi’s sarcoma	C₄₆H₅₈N₄O₉	Advanced or metastatic	Solution (1 mg/1 mL)	Iv	[19,27]
Thiotepa (Thioplex)	Alkalyting agent and is mostly used to treat breast cancer, ovarian cancer, and bladder cancer. It is also used as conditioning for bone marrow transplantation. Its main toxicity is myelosuppression.	C₆H₁₂N₃PS	Advanced or metastatic	Injection, powder, for solution (100 mg; 15 mg; 30 mg)	Ic; Iv; Ives	[28]
Fulvestrant (Faslodex)	Fulvestrant is an estrogen receptor antagonist used to treat HR+ breast cancer that may also be HER2−.	C₃₂H₄₇F₅O₃S	HR+ and HER2− advanced cancer that has not been treated with hormone therapy; HR+ advanced cancer that got worse after treatment with hormone therapy or combined; used with palbociclib or abemaciclib in women with HR+ and HER2− advanced or metastatic cancer that got worse after treatment with hormone therapy	Injection, solution (50 mg/1 mL or 250 mg/5 mL)	Im	[29]
Paclitaxel (Abraxane)	Paclitaxel is a taxoid chemotherapeutic agent isolated from the bark of the Pacific yew tree, used as first-line and subsequent therapy for the treatment of advanced carcinoma of the ovary, and other various cancers including breast and lung cancer.	C₄₇H₅₁NO₁₄	Recurrent or metastatic	Injection, solution (6 mg/1 mL, 30 mg/5 mL, 300 mg/50 mL)	Iv	[16,17,30]
Gemcitabine Hydrochloride(Gemzar)	Gemcitabine is a nucleoside metabolic inhibitor used as adjunct therapy in the treatment of certain types of ovarian cancer, non-small cell lung carcinoma, metastatic breast cancer, and as a single agent for pancreatic cancer.	C₉H₁₁F₂N₃O₄	Combined with paclitaxel in cancer that has not gotten better with other chemotherapy	Injection, solution (38 mg/1 mL, 200 mg/vial, 1 g/vial, 2 g/vial)	Iv	[31]
Letrozole (Femara)	Letrozole is an aromatase inhibitor used to treat breast cancer in postmenopausal women.	C₁₇H₁₁N₅	Early-stage HR+ in women who have already received other treatment; early-stage cancer that has been treated with tamoxifen citrate for at least five years; locally, advanced or metastatic HER2+ and HR+ or HR−; advanced cancer that has gotten worse after anti-estrogen therapy.	Tablet, film coating (2.5 mg)	Oral	[32]
Letrozole (Femara)		C₁₇H₁₁N₅		Letrozole (2.5 mg/L) + Ribociclib succinate (200 mg/L)	Oral	[32]
Olaparib (Lynparza)	Olaparib is a chemotherapeutic agent used to treat recurrent or advanced ovarian cancer and metastatic breast cancer in patients with specific mutations and prior history of chemotherapy.	C₂₄H₂₃FN₄O₃	Metastatic HER2− with certain mutations in the BRCA1 or BRCA2 genes in patients who have been treated with chemotherapy given before or after surgery.	Tablet, film coated (100 mg, 100 mg/L, 150 mg, 150 mg/L)	Oral	[33]
Olaparib (Lynparza)		C₂₄H₂₃FN₄O₃		Capsule (50 mg, 50 mg/L)	Oral
Epirubicin (Ellence)	Epirubicin is an anthracycline topoisomerase II inhibitor used as an adjuvant to treating axillary node metastases in patients who have undergone surgical resection of primary breast cancer.	C₂₇H₂₉NO₁₁	Node-positive breast cancer removed by surgery	Injection, solution (2 mg/1 mL)	Iv	[34]
Eribulin Mesylate (Halaven)	Eribulin is a microtubule inhibitor used to treat metastatic breast cancer and metastatic or unresectable liposarcoma.	C₄₀H₅₉NO₁₁	Patients who have been treated with anthracycline and taxane	Injection, solution (0.44 mg/mL, 0.5 mg/1 mL)	Iv	[35]
Capecitabine (Xeloda)	Capecitabine is an orally-administered chemotherapeutic agent used in the treatment of metastatic breast and colorectal cancers. Capecitabine is a prodrug, that is enzymatically converted to fluorouracil (antimetabolite) in the tumor, where it inhibits DNA synthesis and slows growth of tumor tissue.	C₁₅H₂₂FN₃O₆	Metastatic cancer that has not gotten better with other chemotherapy	Tablet, film coated (150 mg, 500 mg)	Oral	[36]
Ixabepilone (Ixempra)	Ixabepilone is a microtubule inhibitor administered in combination with capecitabine or alone in the treatment of metastatic or locally advanced breast cancer that has shown inadequate response to taxanes and anthracyclines.	C₂₇H₄₂N₂O₅S	Locally advanced or metastatic cancer that has not gotten better with other chemotherapy	Kit (15 mg/15 mg, 45 mg/45 mg)	Iv	[37]
Palbociclib (Ibrance)	Palbociclib is an endocrine-based chemotherapeutic agent used in combination with other antineoplastic agents to treat HER2-negative and HR-positive advanced or metastatic breast cancer.	C₂₄H₂₉N₇O₂	Recurrent or metastatic	Tablet, film coated (75 mg, 100 mg, 125 mg/L)	Oral	[38]
Palbociclib (Ibrance)		C₂₄H₂₉N₇O₂	Recurrent or metastatic	Capsule (75 mg, 75 mg/L, 125 mg/L)	Oral	[38]
Ribociclib (Kisqali)	Ribociclib is a kinase inhibitor used to treat HR+, HER2− advanced or metastatic breast cancer.	C₂₃H₃₀N₈O	Recurrent or metastatic	Tablet, film coated (200 mg, 200 mg/L)	Oral	[39]