Agent

Target(s)

FDA-approved indication(s)

Ado-trastuzumab emtansine (Kadcyla)

HER2 (ERBB2/neu)

• Breast cancer (HER2+)

Afatinib (Gilotrif)

EGFR (HER1/ERBB1), HER2 (ERBB2/neu)

• Non-small cell lung cancer (with EGFR exon 19 deletions or exon 21 substitution (L858R) mutations)

Aldesleukin (Proleukin)

• Renal cell carcinoma
• Melanoma

Alectinib (Alecensa)

ALK

• Non-small cell lung cancer (with ALK fusion)

Alemtuzumab (Campath)

CD52

• B-cell chronic lymphocytic leukemia

Atezolizumab (Tecentriq)

PD-L1

• Urothelial carcinoma
• Non-small cell lung cancer

Avelumab (Bavencio)

PD-L1

• Merkel cell carcinoma
• Urothelial cancer

Axitinib (Inlyta)

KIT, PDGFRβ, VEGFR1/2/3

• Renal cell carcinoma

Belimumab (Benlysta)

BAFF

• Lupus erythematosus

Belinostat (Beleodaq)

HDAC

• Peripheral T-cell lymphoma

Bevacizumab (Avastin)

VEGF ligand

• Cervical cancer
• Colorectal cancer
• Fallopian tube cancer
• Glioblastoma
• Non-small cell lung cancer
• Ovarian cancer
• Peritoneal cancer
• Renal cell carcinoma

Blinatumomab (Blincyto)

CD19/CD3

• Acute lymphoblastic leukemia (precursor B-cell)

Bortezomib (Velcade)

Proteasome

• Multiple myeloma
• Mantle cell lymphoma

Bosutinib (Bosulif)

ABL

• Chronic myelogenous leukemia (Philadelphia chromosome positive)

Brentuximab vedotin (Adcetris)

CD30

• Hodgkin lymphoma
• Anaplastic large cell lymphoma

Brigatinib (Alunbrig)

ALK

• Non-small cell lung cancer (ALK+)

Cabozantinib (Cabometyx [tablet], Cometriq [capsule])

FLT3, KIT, MET, RET, VEGFR2

• Medullary thyroid cancer
• Renal cell carcinoma

Canakinumab (Ilaris)

IL-1β

• Juvenile idiopathic arthritis
• Cryopyrin-associated periodic syndromes

Carfilzomib (Kyprolis)

Proteasome

• Multiple myeloma

Ceritinib (Zykadia)

ALK

• Non-small cell lung cancer (with ALK fusion)

Cetuximab (Erbitux)

EGFR (HER1/ERBB1)

• Colorectal cancer (KRAS wild type)
• Squamous cell cancer of the head and neck

Cobimetinib (Cotellic)

MEK

• Melanoma (with BRAF V600E or V600K mutation)

Crizotinib (Xalkori)

ALK, MET, ROS1

• Non-small cell lung cancer (with ALK fusion or ROS1 gene alteration

Melanoma (with BRAF V600 mutation)

Dabrafenib (Tafinlar)

BRAF

• Melanoma (with BRAF V600 mutation)
• Non-small cell lung cancer (with BRAF V600E mutation)

Daratumumab (Darzalex)

CD38

• Multiple myeloma

Dasatinib (Sprycel)

ABL

• Chronic myelogenous leukemia (Philadelphia chromosome positive)
• Acute lymphoblastic leukemia (Philadelphia chromosome positive)

Denosumab (Xgeva)

RANKL

• Giant cell tumor of the bone

Dinutuximab (Unituxin)

B4GALNT1 (GD2)

• Pediatric neuroblastoma

Durvalumab (Imfinzi)

PD-L1

• Urothelial carcinoma
• Non-small cell lung cancer

Elotuzumab (Empliciti)

SLAMF7 (CS1/CD319/CRACC)

• Multiple myeloma

Enasidenib (Idhifa)

IDH2

• Acute myeloid leukemia (with IDH2 mutation)

Erlotinib (Tarceva)

EGFR (HER1/ERBB1)

• Non-small cell lung cancer (with EGFR exon 19 deletions or exon 21 substitution (L858R) mutations)
• Pancreatic cancer

Everolimus (Afinitor)

mTOR

• Pancreatic, gastrointestinal, or lung origin neuroendocrine tumor
• Renal cell carcinoma
• Nonresectable subependymal giant cell astrocytoma associated with tuberous sclerosis
• Breast cancer (HR+, HER2-)

Gefitinib (Iressa)

EGFR (HER1/ERBB1)

• Non-small cell lung cancer (with EGFR exon 19 deletions or exon 21 substitution (L858R) mutations)

Ibritumomab tiuxetan (Zevalin)

CD20

• Non-Hodgkin's lymphoma

Ibrutinib (Imbruvica)

BTK

• Mantle cell lymphoma
• Chronic lymphocytic leukemia
• Waldenstrom's macroglobulinemia

Idelalisib (Zydelig)

PI3Kδ

• Chronic lymphocytic leukemia
• Follicular B-cell non-Hodgkin lymphoma
• Small lymphocytic lymphoma

Imatinib (Gleevec)

KIT, PDGFR, ABL

• GI stromal tumor (KIT+)
• Dermatofibrosarcoma protuberans
• Multiple hematologic malignancies including Philadelphia chromosome-positive ALL and CML

Ipilimumab (Yervoy)

CTLA-4

• Melanoma
• Renal cell carcinoma

Ixazomib (Ninlaro)

Proteasome

• Multiple Myeloma

Lapatinib (Tykerb)

HER2 (ERBB2/neu), EGFR (HER1/ERBB1)

• Breast cancer (HER2+)

Lenvatinib (Lenvima)

VEGFR2

• Renal cell carcinoma
• Thyroid cancer

Midostaurin (Rydapt)

FLT3

• acute myeloid leukemia (FLT3+)

Necitumumab (Portrazza)

EGFR (HER1/ERBB1)

• Squamous non-small cell lung cancer

Neratinib (Nerlynx)

HER2 (ERBB2/neu)

• Breast cancer (HER2 overexpressed/amplified)

Nilotinib (Tasigna)

ABL

• Chronic myelogenous leukemia (Philadelphia chromosome positive)

Niraparib (Zejula)

PARP

• Ovarian cancer​
• Fallopian tube cancer​
• Peritoneal cancer​

Nivolumab (Opdivo)

PD-1

• Colorectal cancer (dMMR and MSI-H)
• Head and neck squamous cell carcinoma
• Hepatocellular carcinoma
• Hodgkin lymphoma
• Melanoma
• Non-small cell lung cancer
• Renal cell carcinoma
• Urothelial carcinoma

Obinutuzumab (Gazyva)

CD20

• Chronic lymphocytic leukemia
• Follicular lymphoma

Ofatumumab (Arzerra, HuMax-CD20)

CD20

• Chronic lymphocytic leukemia

Olaparib (Lynparza)

PARP

• Ovarian cancer (with BRCA mutation)

Olaratumab (Lartruvo)

PDGFRα

• Soft tissue sarcoma

Osimertinib (Tagrisso)

EGFR

• Non-small cell lung cancer (with EGFR T790M mutation)

Palbociclib (Ibrance)

CDK4, CDK6

• Breast cancer (HR+, HER2-)

Panitumumab (Vectibix)

EGFR (HER1/ERBB1)

• Colorectal cancer (KRAS wild type)

Panobinostat (Farydak)

HDAC

• Multiple myeloma

Pazopanib (Votrient)

VEGFR, PDGFR, KIT

• Renal cell carcinoma

Pembrolizumab (Keytruda)

PD-1

• Classical Hodgkin lymphoma
• Colorectal cancer (MSI-H/dMMR)
• Gastric cancer
• Melanoma
• Non-small cell lung cancer (PD-L1+)
• Head and neck squamous cell carcinoma
• Urothelial cancer
• Solid tumors (MSI-H/dMMR)

Pertuzumab (Perjeta)

HER2 (ERBB2/neu)

• Breast cancer (HER2+)

Ponatinib (Iclusig)

ABL, FGFR1-3, FLT3, VEGFR2

• Chronic myelogenous leukemia
• Acute lymphoblastic leukemia (Philadelphia chromosome positive)

Ramucirumab (Cyramza)

VEGFR2

• Colorectal cancer
• Gastric cancer or Gastroesophageal junction (GEJ) adenocarcinoma
• Non-small cell lung cancer

Regorafenib (Stivarga)

KIT, PDGFRβ, RAF, RET, VEGFR1/2/3

• Colorectal cancer
• Gastrointestinal stromal tumors
• Hepatocellular carcinoma

Ribociclib (Kisqali)

CDK4, CDK6

• Breast cancer (HR+, HER2-)

Rituximab (Rituxan, Mabthera)

CD20

• Non-Hodgkin’s lymphoma
• Chronic lymphocytic leukemia
• Rheumatoid arthritis
• Granulomatosis with polyangiitis

Rituximab/hyaluronidase human (Rituxan Hycela)

CD20

• Chronic lymphocytic leukemia
• Diffuse large B-cell lymphoma
• Follicular lymphoma

Romidepsin (Istodax)

HDAC

• Cutaneous T-cell lymphoma
• Peripheral T-cell lymphoma

Rucaparib (Rubraca)

PARP

• Ovarian cancer (with BRCA mutation)

Ruxolitinib (Jakafi)

JAK1/2

• ​Myelofibrosis

Siltuximab (Sylvant)

IL-6

• Multicentric Castleman's disease

Sipuleucel-T (Provenge)

• Prostate cancer

Sonidegib (Odomzo)

Smoothened

• Basal cell carcinoma

Sorafenib (Nexavar)

VEGFR, PDGFR, KIT, RAF

• Hepatocellular carcinoma
• Renal cell carcinoma
• Thyroid carcinoma

Temsirolimus (Torisel)

mTOR

• Renal cell carcinoma

Tocilizumab (Actemra)

IL-6R

• Rheumatoid arthritis
• Juvenile idiopathic arthritis

Tofacitinib (Xeljanz)

JAK3

• Rheumatoid arthritis

Tositumomab (Bexxar)

CD20

• Non-Hodgkin's lymphoma

Trametinib (Mekinist)

MEK

• Melanoma (with BRAF V600 mutation)
• Non-small cell lung cancer (with BRAF V600E mutation)

Trastuzumab (Herceptin)

HER2 (ERBB2/neu)

• Breast cancer (HER2+)
• Gastric cancer (HER2+)

Vandetanib (Caprelsa)

EGFR (HER1/ERBB1), RET, VEGFR2

• Medullary thyroid cancer

Vemurafenib (Zelboraf)

BRAF

• Melanoma (with BRAF V600 mutation)

Venetoclax (Venclexta)

BCL2

• Chronic lymphocytic leukemia (with 17p deletion)

Vismodegib (Erivedge)

PTCH, Smoothened

• Basal cell carcinoma

Vorinostat (Zolinza)

HDAC

• Cutaneous T-cell lymphoma

Ziv-aflibercept (Zaltrap)

PIGF, VEGFA/B

• Colorectal cancer