Targeted Therapeutics


Kinase Inhibitors
Target Development Name(s) Generic Name(s) Trade
Name(s)
Notes
ABL AMN107 nilotinib Tasigna
AP24534 ponatinib Iclusig
AS703569, R763 cenisertib

AT9283


BMS-354825 dasatinib Sprycel
INNO-406, NS-​187 bafetinib​

SKI-606 bosutinib Bosulif
STI-571, CGP57148, CGP57148B​ imatinib​ Gleevec
XL228

AKT AS703569, R763 cenisertib
catalytic inhibitor
AZD5363

catalytic inhibitor
GDC-0068

catalytic inhibitor​
MK-2206

allosteric inhibitor
ALK
(Anaplastic Lymphoma Kinase)
AP26113


ASP3026


CH5424802, AF802


LDK378


PF-02341066 crizotinib Xalkori
TSR-011


X-396


Aurora A AS703569, R763 cenisertib

AT9283


ENMD-2076


MK5108


MLN8237 alisertib

PF-03814735


TAK901


Aurora B AS703569, R763 cenisertib

AT9283


AZD1152-HQPA, AZD1152 barasertib


GSK1070916


PF-03814735


Aurora C GSK1070916


Aurora A/B/C AMG900


BI 847325


PHA-739358 danusertib

SNS-314


BRAF ARQ 736


GSK2118436 dabrafenib

PLX-4032, RG7204, R05185426 vemurafenib Zelboraf
RAF265


RO5212054, PLX3603


BTK AS703569, R763 cenisertib

PCI-32765 ibrutinib

CDK 1,2,4,5,6,7,9 (pan-CDK) HMR-1275, L868275, flavopiridol alvocidib

CDK 1,2,5,9 SCH727965 dinaciclib

CDK 2,7,9 CYC202 seliciclib

CDK 4,6 LEE011


LY2835219


PD 0332991 palbociclib

CSF-1R PLX3397, PLX108-01


EGFR (HER1/ERBB1) AEE788, NVP-AEE788


AP26113


AZD6474, ZD6474 vandetanib Zactima, Caprelsa
BIBW-2992 afatinib Tomtovok
BPI-2009H icotinib

CI-1033, PD183805 canertinib

CO-1686


HMPL-813 epitinib


MNPL-309 theliatinib

OSI-774, CP-258,774 erlotinib Tarceva
XL647, KD019


ZD1839 gefitinib Iressa
EGFR (HER1/ERBB1)
HER2 (ERBB2/neu)
HER3 (ERBB3)
AZD8931


EGFR (HER1/ERBB1)
HER2 (ERBB2/neu)
HER4 (ERBB4)
BMS-599626, AC480


BMS-690514, EVRI


EKB-569 pelitinib

PF-00299804 dacomitinib

EphB4 XL647, KD019


FAK AB1010 masitinib Masivet
FGFR1/2/3 AB1010 masitinib Masivet
AP24534 ponatinib Iclusig
AZD4547


BGJ398, NVP-BGJ398


BIBF1120 nintedanib Vargatef
E-3810


HMPL-012 sulfatinib

TKI258, CHIR-258 dovitinib

XL228

FGFR1 TSU 68, SU6668 orantinib

FGFR3 ENMD-2076


FLT3 AC220 quizartinib

AP24534 ponatinib Iclusig
AS703569, R763 cenisertib

CEP-701 lestaurtinib

ENMD-0276


MLN518, CT53518 tandutinib

MP-470 amuvatinib

PKC412 midostaurin

PLX3397, PLX108-01


SU-11248 sunitinib Sutent
XL184 cabozantinib Cometriq
HER2 (ERBB2/neu) AEE788, NVP-AEE788


ARRY 380


BIBW-2992 afatinib Tomtovok
CI-1033, PD183805 canertinib

GSK572016, GW2016, GW-572016 lapatinib Tykerb
HKI-272 neratinib

TAK 165 mubritinib

XL647, KD019


IGF-1R BMS-536924


BMS-754807


OSI-906 ​linsitinib

XL228

JAK1/2 AZD1480


CYT-387 momelotinib

INCB18424 ruxolitinib Jakafi
JAK2 AT9283


BMS-911543


CEP-701 lestaurtinib

SAR302503, TG101348


SB1518 pacritinib

XL019


JAK2 V617F SB1518 pacritinib

LY2784544


XL019


JAK3 CP-690550 tofacitinib citrate Xeljanz
KIT AB1010 masitinib Masivet
AG-013736 axitinib Inlyta
AMG706 motesanib

AS703569, R763 cenisertib

BAY 57-9352 telatinib

BAY 73-4506 regorafenib Stivarga
BMS-354825 dasatinib Sprycel
GW786034 pazopanib Votrient
MLN518, CT53518 tandutinib

MP-470 amuvatinib

PKC412 midostaurin

PLX3397, PLX108-01


STI-571, CGP57148, CGP57148B imatinib Gleevec
SU-11248 sunitinib Sutent
XL184 cabozantinib Cometriq
XL820


LYN INNO-406, NS-187 bafetinib

AS703569, R763 cenisertib

MEK AS703026, MSC1936369B pimasertib

AZD6244, ARRY-142886 selumetinib

AZD8330


BAY 86-9766, RDEA119 refametinib

BI 847325


CI-1040


GDC-0623


GDC-0973


GSK1120212 trametinib

MEK162


PD0325901, PD-0325901


TAK-733


MET AMG 208

ARQ 197 tivantinib

BMS-777607


EMD 1214063


EXEL-2880, GSK1363089, XL880 foretinib

HMPL-504 volitinib

INCB028060, INC280


MGCD265


MK-2461


MP-470 amuvatinib

PF-02341066 crizotinib Xalkori
PF-04217903


XL184 cabozantinib Cometriq
mTOR AP23573, MK8669 ridaforolimus (deforolimus)
rapalogue​
AY 22989, SILA 9268A, WY-090217 sirolimus Rapamune rapalogue​​
AZD8055

TORC1/2, catalytic inhibitor​
BEZ235, NVP-BEZ235

catalytic, dual PI3K/mTOR inhibitor
BGT226, NVP-BGT226

dual PI3K/mTOR inhibitor
CCI-779 temsirolimus Torisel rapalogue​
GDC-0980

catalytic, dual PI3K/mTOR inhibitor
MLN0128, INK128

TORC1/2, catalytic inhibitor​
OSI-027

TORC1/2, catalytic inhibitor​
PF-4691502

catalytic, dual PI3K/mTOR inhibitor
PI-103

catalytic, dual PI3K/mTOR inhibitor
PKI-587

pan-PI3K inhibitor, catalytic, dual PI3K/mTOR inhibitor
PWT33597

catalytic, dual PI3K/mTOR inhibitor
RAD001 everolimus Afinitor rapalogue​
SF1126

catalytic, dual PI3K/mTOR inhibitor
XL-765

catalytic, dual PI3K/mTOR inhibitor
PDGFR AMG706 motesanib

BIBF1120 nintedanib Vargatef
GW786034 pazopanib Votrient
MLN518, CT53518 tandutinib

X-82

inhibits all isoforms
PDGFRα CP-868569 crenolanib

MP-470 amuvatinib

PKC412 midostaurin

PDGFRβ ABT-869 linifanib

AG-013736 axitinib Inlyta
BAY 43-9006 sorafenib Nexavar
BAY 57-9352 telatinib

BAY 73-4506 regorafenib Stivarga
SU-11248 sunitinib Sutent
TSU 68, SU6668 orantinib

XL820


PI3K BAY 80-6946

pan-PI3K inhibitor
BEZ235, NVP-BEZ235

catalytic, dual PI3K/mTOR inhibitor
BGT226, NVP-BGT226

dual PI3K/mTOR inhibitor
BKM120

pan-PI3K inhibitor
BYL719


GDC-0941

pan-PI3K inhibitor
GDC-0980

catalytic, dual PI3K/mTOR inhibitor
GSK2636771


PF-4691502

catalytic, dual PI3K/mTOR inhibitor
PI-103

catalytic, dual PI3K/mTOR inhibitor
PKI-587

pan-PI3K inhibitor, catalytic
PWT33597

catalytic, dual PI3K/mTOR inhibitor
PX-866


SF1126

catalytic, dual PI3K/mTOR inhibitor
XL147, SAR245408

pan-PI3K inhibitor
XL-765

catalytic, ​dual PI3K/mTOR inhibitor

sophoretin, quercetin

PI3Kα BYL719


GDC-0032


INK-1117


PI3Kδ CAL-101, GS-1101


PKC
sophoretin, quercetin

PKCα LY317615 enzastaurin

PKC412 midostaurin

PKCβ LY317615 enzastaurin

PKCγ LY317615 enzastaurin

PKCε LY317615 enzastaurin

PLK1 BI 6727 volasertib

BI 2536


GSK461364, GSK-461364


NMS-1286937


ON 01910.Na rigosertib Estybon
RAF BAY 43-9006 sorafenib Nexavar
BAY 73-4506 regorafenib Stivarga
LGX818


XL281, BMS-908662


RET AMG706 motesanib

AZD6474, ZD6474 vandetanib Zactima, Caprelsa
BAY 43-9006 sorafenib Nexavar
BAY 73-4506 regorafenib Stivarga
MP-470 amuvatinib

SU-11248 sunitinib Sutent
XL184 cabozantinib Cometriq
ROS1 PF-02341066 crizotinib Xalkori
SCFR AB1010 masitinib Masivet
SRC AZD0530 saracatinib

BMS-354825 dasatinib Sprycel
KX2-391


XL228

SYK R788 fostamatinib

TORC1/2 AZD8055

catalytic inhibitor​
MLN0128, INK128

catalytic inhibitor​
OSI-027

catalytic inhibitor​
VEGFR ABT-869 linifanib

ENMD-2076


EXEL-2880, GSK1363089, XL880 foretinib

HMPL-012 sulfatinib

PTK 787, CGP 79787, ZK 222584 vatalanib

TSU 68, SU6668 orantinib

X-82

inhibits all isoforms
XL647, KD019


VEGFR1/2/3 AG-013736 axitinib Inlyta
AMG706 motesanib

BAY 73-4506 regorafenib Stivarga
BIBF1120 nintedanib Vargatef
E-3810


GW786034 pazopanib Votrient
HMPL-013 fruquintinib

KRN951, AV-951 tivozanib

MGCD265


VEGFR2 AEE788, NVP-AEE788


AP24534 ponatinib Iclusig
AZD2171 cediranib Recentin
AZD6474, ZD6474 vandetanib Zactima, Caprelsa
BAY 43-9006 sorafenib Nexavar
BMS-582664 brivanib

BMS-690514, EVRI


E7080 lenvatinib

PKC412 midostaurin

RAF265


SU-11248 sunitinib Sutent
XL184 cabozantinib Cometriq
XL820


YN968D1 apatinib

VEGFR2/3 BAY 57-9352 telatinib

E7080 lenvatinib


Therapeutic Antibodies
Target Development Name(s) Generic Name(s) Trade
Name(s)
Notes
BAFF
belimumab Benlysta
CCR4 KW-0761 mogamulizumab

CD19/CD3 MT103, MT-103, MEDI-538 blinatumomab

CD20 IDEC-102, IDEC-C2B8 rituximab Rituxan, Mabthera
IDEC Y2B8 ibritumomab tiuxetan Zevalin drug can be bound via tiuxetan to 111In or 90Y

ofatumumab Arzerra, HuMax-CD20
CD22 CAT-8015 moxetumomab pasudotox

CD30 SGN-35 brentuximab Adcetris
CD38
daratuzumab HuMax-CD38
CD52 Campath alemtuzumab

CD56 IMGN901 lorvotuzumab mertansine

CD74 hLL1 milatuzumab

CTLA4 CP675,206 tremelimumab
MDX-010, MDX-101, BMS-734016 ipilimumab Yervoy
EGFL7 MEGF0444A


EGFR (HER1/ERBB1) ABT-806, mAb-806


ABX-EGF panitumumab Vectibix
h-R3, TheraCIM nimotuzumab

IMC-11F8 necitumumab

IMC-C225 cetuximab Erbitux
MEHD7945 A


MM-151


RO5083945, GA201


Sym004


FZD7 OMP-18R5 vantictumab

HER2 (ERBB2/neu) MM-111


MOAB 2C4 pertuzumab Perjeta, Omnitarg
PRO132365 ado-trastuzumab emtansine, T-DM1 Kadcyla

trastuzumab Herceptin
HER3 (ERBB3) AV 203


MEHD7945 A


MM-111


MM-121, SAR256212


U3-1287, AMG 888


HGF AMG 102 rilotumumab

AV-299, SCH900105 ficlatuzumab

IGF-1R AMG-479 ganitumab

BI 836845


BIIB022


CP-751871 figitumumab

IMC-A12 cixutumumab

MEDI-573


MK-0646 dalotuzumab

IGF-2R BI 836845


MEDI-573


MET LY2875358


MetMAb, R05490258, OA-5D onartuzumab

PD-1 AMP-224


BMS-936558, MDX-1106, ONO-4538 nivolumab

CT-011 pidilizumab

MK-3475


PD-L1 MDX-1105, BMS-936559


MPDL3280A, RG7446


PDGFRα IMC-3G3 ramucirumab

MEDI-575


PIGF
ziv-aflibercept Zaltrap
TRAIL-R1/DR4,R2/D5 AMG951, rhApo2L/TRAIL dulanermin

TRAIL-R1/D4 HGS-ETR1 mapatumumab

TRAIL-R2/D5 AMG-655 conatumumab

HGS-ETR2 lexatumumab

LBY135


PRO95780 apomab

VEGFA
bevacizumab Avastin

ziv-aflibercept Zaltrap
VEGFB
ziv-aflibercept Zaltrap
VEGFR2 IMC-1121B ramucirumab


Immunotherapies
Target Development Name(s) Generic Name(s) Trade
Name(s)
Notes
CTLA4 CP675,206 tremelimumab
MDX-010, MDX-101, BMS-734016 ipilimumab Yervoy
IL-6
siltuximab

IL-6R R-1569 tocilizumab Actemra
IL-1β ACZ885 canakinumab Ilaris
PD-1 AMP-224


BMS-936558, MDX-1106, ONO-4538 nivolumab

CT-011 pidilizumab

MK-3475


PD-L1 MDX-1105, BMS-936559


MPDL3280A, RG7446


Other
interferon-alpha

APC8015 sipuleucel-T Provenge
TheraCys BCG vaccine

TSF aldesleukin Proleukin

Chemotherapies
Type of Chemotherapy Subtype Generic Name(s) Trade
Name(s)
Notes
Alkylating Agents Nitrogen mustard bendamustine Treanda, Ribomustin
chlorambucil Ambochlorin
cyclophosphamide Clafen
ifosfamide Cyfos
melphalan Alkeran
palifosfamide tris

Ethylenimines thiotepa Girostan
Nitrosoureas carmustine Becenum
lomustine CeeNU
streptozocin Zanosar
Alkyl sufonates busulfan Busulfex
Triazenes dacarbazine DTIC-Dome
temozolomide Methazolastone
Platinum analogues carboplatin Paraplat
cisplatin Platinol
oxaliplatin Eloxatin
Other procarbazine Matulane
Topoisomerase II inhibitors Anthracyclines daunorubicin Cerubidine
liposomal daunorubicin DaunoXome
doxorubicin Adriamycin PFS
liposomal doxorubicin Doxil
epirubicin Ellence
idarubicin Idamycin
valrubicin Valstar
Epipodophyllotoxins etoposide/etoposide phosphate Toposar
teniposide Vumon
Anthracenedione mitoxantrone Novantrone
Other amonafide

Topoisomerase I inhibitors Camptothecin derivatives etirinotecan

irinotecan Camptosar
topotecan Hycamptin
Quinoline alkaloids camptothecin

Antimicrotubule Agents Epothilones ixabepilone Ixempra
Vinca alkaloids vinblastine Velban, Velsar
vincristine Vincasar PFS
liposomal vincristine Marqibo
vinorelbine Navelbine
Taxanes paclitaxel Taxol
albumin-bound paclitaxel, nab-paclitaxel Abraxane
docetaxel Taxotere
cabazitaxel Jevtana
Halichondrin B analogue eribulin mesylate

Antimetabolites Folate antagonists methotrexate Abitrexate
pemetrexed Alimta
pralatrexate Folotyn
raltitrexed Tomudex
Purine analogues cladribine Leustatin
clofarabine Clofarex
fludarabine Fludara
mercaptopurine Mercaptopurinum
nelarabine Arranon
pentostatin Nipent
thioguanine Tabloid
Pyrimidine analogues capecitabine Xeloda
cytarabine Cytosar-U
floxuridine FUDF
fluorouracil Adrucil
gemcitabine Gemzar
Other hydroxyurea Droxia
Other Antitumor antibiotic bleomycin Blenoxane
dactinomycin Cosmegen
mitomycin Mitozytrex
Aspariginase derivatives e. coli derived asparaginase Cristanaspase
erwinia derived asparaginase Erwinaze
pegaspargase Oncaspar
Hypomethylating Agents azacitidine Mylosar
decitabine Dacogen
Retinoic acid derivatives alitretinoin Panretin
bexarotene Targretin
tretinoin Aberel
Telomerase template antagonist imetelstat

Other arsenic trioxide Trisenox

mitotane Lysodren
trabectedin Yondelis
denileukin diftitox Ontak
octreotide Sandostatin
dexamethasone/prednisone Aeroseb-Dex

Hormonal Agents
Type of Agent Development Name Generic Name(s) Trade
Name(s)
Notes
Selective androgen receptor modulator (SARM) GTX-024 enobosarm Osterine
Androgen receptor antagonist
nilutamide Nilandron, Anandron

bicalutamide Casodex

flutamide Eulexin, Apimid
MDV3100 enzalutamide Xtandi
Aromatase inhibitor CGS 20267 letrozole Femara
FCE-24304 exemestane Aromasin

anastrozole Arimidex
Estrogen receptor antagonist
fulvestrant Faslodex
Selective estrogen receptor modulator (SERM)
tamoxifen Nolvadex
LY-139481 raloxifene Evista, Keoxifene

toremifene Fareston
LH-RH analogues and antagonists
degarelix Firmagon

leuprolide Lupron

triptorelin Decapeptyl

goserelin Zoladex
Other
abiraterone


megestrol acetate


estramustine Emcyt, Estracyt

ketoconazole


Other
Target Development Name(s) Generic Name(s) Trade
Name(s)
Notes
Ang1/Ang2 AMG 386 trebananib

Bcl-2 ABT-263, ABT-737 navitoclax

AT101


GX15-070 obatoclax

G3139 oblimerson Genasense
CXCR4 LY2510924


Farnesyl protein transferase (FTase) IND 58359 tipifarnib Zarnestra
Gamma-secretase MK0752


HDAC FK228 romidepsin Istodax
LBH589 panobinostat Faridak
MK-0683 vorinostat Zolinza
MS-275, SNDX-275 entinostat

PXD101 belinostat

HSP90 17-AAG, KOS-953 tanespimycin

AT13387


AUY922


Debio 0932


IPI-504 retaspimycin

STA-9090 ganetespib

Notch Pathway MK0752


PF-03084014


REGN421


RO4929097, R4733


PARP ABT-888 veliparib

AG-014699 , PF-01367338 rucaparib

AZD2281 olaparib

BSI-201 iniparib

MK4827


PPAR-γ CS 7017, RS5444


Proteasome LDP 341, MLN341, PS-341 bortezomib Velcade
PR-171 carfilzomib Kyprolis
PTCH GDC-0449 vismodegib Erivedge
Smoothened GDC-0449 vismodegib Erivedge
LDE225 erismodegib

LY2940680


Other CC-4047 pomalidomide Pomalyst thalidomide derivative
CC-5013 lenalidomide Revlimid thalidomide analog

thalidomide Thalomid

​​​​​​​​​​​​​​​​​​

NOTE: To suggest additions or changes, please contact us here.​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​

Authors: Jonathan L. Aston, Pharm.D., Christine Lovly, M.D., Ph.D.

Last Updated: April 29, 2013

Disclaimer: The information presented at MyCancerGenome.org is compiled from sources believed to be reliable. Extensive efforts have been made to make this information as accurate and as up-to-date as possible. However, the accuracy and completeness of this information cannot be guaranteed. Despite our best efforts, this information may contain typographical errors and omissions. The contents are to be used only as a guide, and health care providers should employ sound clinical judgment in interpreting this information for individual patient care.