| osimertinib Approved |
EGFR TKI (3rd generation) |
EGFR exon 19 deletion / L858R, EGFR exon 20 insertion, RET fusion or mutation, ALK fusion, PIK3CA activating mutation, BRCA1/2 mutation, KRAS G12C, KRAS G12D, MET exon 14 skipping |
123 |
| cetuximab Approved |
anti-EGFR antibody |
KRAS G12C, KRAS G12D, BRAF V600E, MSI-H / dMMR, ALK fusion, EGFR exon 19 deletion / L858R, NTRK1/2/3 fusion, PIK3CA activating mutation, RET fusion or mutation, EGFR exon 20 insertion, HER2 (ERBB2) activating mutation, MET exon 14 skipping |
83 |
| olaparib Approved |
PARP inhibitor |
BRCA1/2 mutation, IDH1/2 mutation, HER2-low / ultralow (IHC 1+ or 2+/ISH-), MSI-H / dMMR, FGFR2 fusion or rearrangement, FGFR3 alteration (mutation or fusion), HER2 (ERBB2) activating mutation, KRAS G12C, KRAS G12D, PIK3CA activating mutation, BRAF V600E, EGFR exon 19 deletion / L858R |
47 |
| venetoclax |
BCL-2 inhibitor |
FLT3 mutation (ITD/TKD), NPM1 mutation, IDH1/2 mutation, KRAS G12C, KRAS G12D, ALK fusion |
43 |
| trametinib Approved |
MEK inhibitor |
BRAF V600E, KRAS G12C, KRAS G12D, NTRK1/2/3 fusion, ALK fusion, EGFR exon 19 deletion / L858R, RET fusion or mutation, ROS1 fusion, EGFR exon 20 insertion, MET exon 14 skipping, MSI-H / dMMR |
42 |
| furmonertinib |
EGFR TKI (3rd generation) |
EGFR exon 19 deletion / L858R, EGFR exon 20 insertion, HER2 (ERBB2) activating mutation |
36 |
| dabrafenib Approved |
BRAF inhibitor |
BRAF V600E, NTRK1/2/3 fusion, ALK fusion, KRAS G12C, RET fusion or mutation, ROS1 fusion, EGFR exon 20 insertion, KRAS G12D, MSI-H / dMMR |
33 |
| encorafenib Approved |
BRAF inhibitor |
BRAF V600E, MSI-H / dMMR, ALK fusion, KRAS G12C, KRAS G12D |
32 |
| ivosidenib Approved |
IDH1 inhibitor |
IDH1/2 mutation, FLT3 mutation (ITD/TKD), FGFR2 fusion or rearrangement |
27 |
| gilteritinib Approved |
FLT3 inhibitor |
FLT3 mutation (ITD/TKD), NPM1 mutation, ALK fusion, IDH1/2 mutation, EGFR exon 19 deletion / L858R |
24 |
| amivantamab Approved |
EGFR-MET bispecific antibody |
EGFR exon 19 deletion / L858R, EGFR exon 20 insertion, MET exon 14 skipping, ALK fusion, IDH1/2 mutation, KRAS G12C, MSI-H / dMMR, ROS1 fusion |
23 |
| trastuzumab |
anti-HER2 antibody |
HER2-low / ultralow (IHC 1+ or 2+/ISH-), MSI-H / dMMR, PIK3CA activating mutation, HER2 (ERBB2) activating mutation, BRCA1/2 mutation, Claudin 18.2 expression, EGFR exon 19 deletion / L858R, KRAS G12C, KRAS G12D, ALK fusion, BRAF V600E, FGFR2 fusion or rearrangement, FGFR3 alteration (mutation or fusion), MET exon 14 skipping, RET fusion or mutation |
23 |
| aumolertinib |
EGFR TKI (3rd generation) |
EGFR exon 19 deletion / L858R, ALK fusion, BRAF V600E, BRCA1/2 mutation, EGFR exon 20 insertion, HER2-low / ultralow (IHC 1+ or 2+/ISH-), ROS1 fusion |
22 |
| binimetinib Approved |
MEK inhibitor |
BRAF V600E, KRAS G12D, MSI-H / dMMR, KRAS G12C, ALK fusion, EGFR exon 19 deletion / L858R, ROS1 fusion |
22 |
| lorlatinib Approved |
ALK TKI (3rd generation) |
ALK fusion, ROS1 fusion, BRAF V600E, EGFR exon 19 deletion / L858R, KRAS G12C, KRAS G12D |
21 |
| sotorasib Approved |
KRAS G12C inhibitor (OFF state) |
KRAS G12C, EGFR exon 19 deletion / L858R, KRAS G12D, MSI-H / dMMR, BRAF V600E |
21 |
| adagrasib Approved |
KRAS G12C inhibitor (OFF state) |
KRAS G12C, BRAF V600E, KRAS G12D, EGFR exon 19 deletion / L858R |
17 |
| alectinib Approved |
ALK TKI (2nd generation) |
ALK fusion, ROS1 fusion, BRAF V600E, NTRK1/2/3 fusion, BRCA1/2 mutation, EGFR exon 19 deletion / L858R, KRAS G12C, RET fusion or mutation, MSI-H / dMMR, PIK3CA activating mutation |
17 |
| crizotinib Approved |
ALK/ROS1 TKI (1st generation) |
ALK fusion, ROS1 fusion, BRAF V600E, BRCA1/2 mutation, EGFR exon 19 deletion / L858R, EGFR exon 20 insertion, KRAS G12C, MET exon 14 skipping, MSI-H / dMMR, NTRK1/2/3 fusion, RET fusion or mutation, KRAS G12D |
17 |
| abemaciclib Approved |
CDK4/6 inhibitor |
PIK3CA activating mutation, ESR1 mutation, IDH1/2 mutation, BRCA1/2 mutation, KRAS G12C, BRAF V600E, EGFR exon 19 deletion / L858R, HER2-low / ultralow (IHC 1+ or 2+/ISH-), KRAS G12D, ALK fusion, MSI-H / dMMR |
16 |
| lazertinib Approved |
EGFR TKI (3rd generation) |
EGFR exon 19 deletion / L858R, EGFR exon 20 insertion, MET exon 14 skipping |
16 |
| inavolisib Approved |
PI3Kα inhibitor |
PIK3CA activating mutation, BRCA1/2 mutation, HER2 (ERBB2) activating mutation, KRAS G12C, ALK fusion, BRAF V600E, MSI-H / dMMR, RET fusion or mutation |
15 |
| palbociclib Approved |
CDK4/6 inhibitor |
PIK3CA activating mutation, BRCA1/2 mutation, ESR1 mutation, ALK fusion, BRAF V600E, EGFR exon 19 deletion / L858R, KRAS G12C, KRAS G12D, ROS1 fusion, FGFR2 fusion or rearrangement, FGFR3 alteration (mutation or fusion) |
15 |
| sunvozertinib Approved |
EGFR exon 20 insertion TKI |
EGFR exon 20 insertion, EGFR exon 19 deletion / L858R, ALK fusion, BRAF V600E, HER2 (ERBB2) activating mutation, KRAS G12C, NTRK1/2/3 fusion, RET fusion or mutation, ROS1 fusion |
15 |
| ensartinib Approved |
ALK TKI (2nd generation) |
ALK fusion, ROS1 fusion, BRAF V600E, EGFR exon 20 insertion, KRAS G12C, MET exon 14 skipping, NTRK1/2/3 fusion, RET fusion or mutation |
14 |
| panitumumab Approved |
anti-EGFR antibody |
KRAS G12C, KRAS G12D, BRAF V600E, BRCA1/2 mutation, MSI-H / dMMR |
14 |
| ribociclib |
CDK4/6 inhibitor |
PIK3CA activating mutation, BRAF V600E, ESR1 mutation, ALK fusion, BRCA1/2 mutation, EGFR exon 19 deletion / L858R, HER2-low / ultralow (IHC 1+ or 2+/ISH-), KRAS G12C, KRAS G12D, NTRK1/2/3 fusion, ROS1 fusion, IDH1/2 mutation |
14 |
| vemurafenib Approved |
BRAF inhibitor |
BRAF V600E, ALK fusion, ROS1 fusion, BRCA1/2 mutation, EGFR exon 19 deletion / L858R, KRAS G12C, NTRK1/2/3 fusion, RET fusion or mutation, KRAS G12D, MSI-H / dMMR, PIK3CA activating mutation |
14 |
| zolbetuximab Approved |
anti-CLDN18.2 antibody |
Claudin 18.2 expression, MSI-H / dMMR |
14 |
| alpelisib Approved |
PI3Kα inhibitor |
PIK3CA activating mutation, ALK fusion, BRAF V600E, BRCA1/2 mutation, HER2 (ERBB2) activating mutation |
13 |
| daraxonrasib |
RAS(ON) multi-selective inhibitor |
KRAS G12D, KRAS G12C |
13 |
| enasidenib Approved |
IDH2 inhibitor |
IDH1/2 mutation, FLT3 mutation (ITD/TKD) |
13 |
| niraparib Approved |
PARP inhibitor |
BRCA1/2 mutation, IDH1/2 mutation, ALK fusion, BRAF V600E, EGFR exon 19 deletion / L858R, ROS1 fusion, MSI-H / dMMR |
13 |
| selpercatinib Approved |
RET inhibitor |
RET fusion or mutation, BRAF V600E, ALK fusion, EGFR exon 19 deletion / L858R, MET exon 14 skipping, NTRK1/2/3 fusion, ROS1 fusion |
13 |
| vebreltinib |
MET TKI |
EGFR exon 19 deletion / L858R, MET exon 14 skipping, IDH1/2 mutation |
13 |
| afatinib Approved |
EGFR TKI (2nd generation) |
EGFR exon 19 deletion / L858R, KRAS G12C, FGFR2 fusion or rearrangement, FGFR3 alteration (mutation or fusion), HER2 (ERBB2) activating mutation, HER2-low / ultralow (IHC 1+ or 2+/ISH-), MSI-H / dMMR, EGFR exon 20 insertion, KRAS G12D, NRG1 fusion |
12 |
| erdafitinib Approved |
FGFR inhibitor |
FGFR3 alteration (mutation or fusion), FGFR2 fusion or rearrangement, MSI-H / dMMR |
12 |
| glecirasib |
KRAS G12C inhibitor (OFF state) |
KRAS G12C, ALK fusion, BRAF V600E, EGFR exon 20 insertion, NTRK1/2/3 fusion, RET fusion or mutation, ROS1 fusion |
12 |
| revumenib Approved |
menin inhibitor |
NPM1 mutation, FLT3 mutation (ITD/TKD) |
12 |
| vorasidenib Approved |
brain-penetrant IDH1/2 inhibitor |
IDH1/2 mutation |
11 |
| calderasib |
KRAS G12C inhibitor (OFF state) |
KRAS G12C, KRAS G12D, MSI-H / dMMR |
10 |
| capivasertib Approved |
AKT inhibitor |
PIK3CA activating mutation, HER2-low / ultralow (IHC 1+ or 2+/ISH-), EGFR exon 19 deletion / L858R, MSI-H / dMMR, BRCA1/2 mutation |
10 |
| cobimetinib Approved |
MEK inhibitor |
BRAF V600E, ALK fusion, KRAS G12C, KRAS G12D, NTRK1/2/3 fusion, RET fusion or mutation, ROS1 fusion, BRCA1/2 mutation, EGFR exon 19 deletion / L858R, MSI-H / dMMR, PIK3CA activating mutation |
10 |
| defactinib Approved |
FAK inhibitor |
KRAS G12C, KRAS G12D, ALK fusion, BRAF V600E, IDH1/2 mutation, MSI-H / dMMR, NTRK1/2/3 fusion, RET fusion or mutation |
10 |
| erlotinib Approved |
EGFR TKI (1st generation) |
EGFR exon 19 deletion / L858R, KRAS G12C, ALK fusion, KRAS G12D, BRAF V600E, HER2 (ERBB2) activating mutation, RET fusion or mutation, EGFR exon 20 insertion, PIK3CA activating mutation, ROS1 fusion |
10 |
| garsorasib |
KRAS G12C inhibitor (OFF state) |
KRAS G12C |
10 |
| olutasidenib Approved |
IDH1 inhibitor |
IDH1/2 mutation, FLT3 mutation (ITD/TKD) |
10 |
| avutometinib Approved |
RAF/MEK clamp |
KRAS G12C, KRAS G12D, ALK fusion, BRAF V600E, IDH1/2 mutation, NTRK1/2/3 fusion, RET fusion or mutation |
9 |
| befotertinib |
EGFR TKI (3rd generation) |
EGFR exon 19 deletion / L858R, EGFR exon 20 insertion |
9 |
| limertinib |
EGFR TKI (3rd generation) |
EGFR exon 19 deletion / L858R |
9 |
| pemigatinib Approved |
FGFR inhibitor |
FGFR2 fusion or rearrangement, FGFR3 alteration (mutation or fusion), FLT3 mutation (ITD/TKD), IDH1/2 mutation, MSI-H / dMMR |
9 |
| PLB1004 |
EGFR TKI (incl. exon 20 insertions) |
EGFR exon 19 deletion / L858R, EGFR exon 20 insertion, HER2 (ERBB2) activating mutation |
9 |
| talazoparib Approved |
PARP inhibitor |
BRCA1/2 mutation, KRAS G12C, KRAS G12D, MSI-H / dMMR, IDH1/2 mutation |
9 |
| VS-7375 |
KRAS G12D inhibitor (ON/OFF) |
KRAS G12D |
9 |
| ziftomenib Approved |
menin inhibitor |
NPM1 mutation, FLT3 mutation (ITD/TKD) |
9 |
| entrectinib Approved |
TRK/ROS1 TKI |
ROS1 fusion, ALK fusion, NTRK1/2/3 fusion, BRAF V600E, KRAS G12C, RET fusion or mutation, BRCA1/2 mutation |
8 |
| fulzerasib |
KRAS G12C inhibitor (OFF state) |
KRAS G12C, KRAS G12D |
8 |
| larotrectinib Approved |
TRK inhibitor |
NTRK1/2/3 fusion, BRAF V600E, RET fusion or mutation, ALK fusion, EGFR exon 20 insertion, KRAS G12C, ROS1 fusion |
8 |
| savolitinib |
MET TKI |
EGFR exon 19 deletion / L858R, ALK fusion, BRAF V600E, EGFR exon 20 insertion, KRAS G12C, MET exon 14 skipping, NTRK1/2/3 fusion, RET fusion or mutation, ROS1 fusion, MSI-H / dMMR |
8 |
| zoldonrasib |
KRAS G12D inhibitor (ON state) |
KRAS G12D, KRAS G12C |
8 |
| HRS-4642 |
KRAS G12D inhibitor |
KRAS G12D, KRAS G12C |
7 |
| ifebemtinib |
FAK inhibitor |
KRAS G12C, EGFR exon 19 deletion / L858R, KRAS G12D |
7 |
| pertuzumab |
anti-HER2 antibody |
PIK3CA activating mutation, MSI-H / dMMR, BRCA1/2 mutation, HER2 (ERBB2) activating mutation, HER2-low / ultralow (IHC 1+ or 2+/ISH-), ALK fusion, BRAF V600E, RET fusion or mutation |
7 |
| selumetinib |
MEK inhibitor |
KRAS G12C, KRAS G12D, EGFR exon 19 deletion / L858R, BRAF V600E, FGFR2 fusion or rearrangement, FGFR3 alteration (mutation or fusion) |
7 |
| tucatinib |
HER2 TKI |
HER2-low / ultralow (IHC 1+ or 2+/ISH-), HER2 (ERBB2) activating mutation, EGFR exon 19 deletion / L858R, PIK3CA activating mutation, BRAF V600E |
7 |
| brigatinib Approved |
ALK TKI (2nd generation) |
ALK fusion, ROS1 fusion |
6 |
| divarasib |
KRAS G12C inhibitor (OFF state) |
KRAS G12C, ALK fusion, BRAF V600E, NTRK1/2/3 fusion, RET fusion or mutation, ROS1 fusion |
6 |
| gefitinib Approved |
EGFR TKI (1st generation) |
EGFR exon 19 deletion / L858R, EGFR exon 20 insertion |
6 |
| pyrotinib |
HER2 TKI |
HER2-low / ultralow (IHC 1+ or 2+/ISH-), ALK fusion, BRAF V600E, ROS1 fusion, BRCA1/2 mutation, EGFR exon 19 deletion / L858R, EGFR exon 20 insertion, HER2 (ERBB2) activating mutation, KRAS G12C, NTRK1/2/3 fusion, RET fusion or mutation |
6 |
| quizartinib Approved |
FLT3 inhibitor |
FLT3 mutation (ITD/TKD), NPM1 mutation |
6 |
| rituximab |
anti-CD20 antibody |
BRAF V600E, FLT3 mutation (ITD/TKD), ALK fusion, IDH1/2 mutation |
6 |
| zongertinib Approved |
HER2 TKI |
HER2 (ERBB2) activating mutation |
6 |
| adavosertib |
WEE1 inhibitor |
BRCA1/2 mutation, FGFR2 fusion or rearrangement, FGFR3 alteration (mutation or fusion), MSI-H / dMMR, BRAF V600E, FLT3 mutation (ITD/TKD) |
5 |
| dacomitinib Approved |
EGFR TKI (2nd generation) |
EGFR exon 19 deletion / L858R, ALK fusion, BRAF V600E, BRCA1/2 mutation, ROS1 fusion, KRAS G12C, KRAS G12D |
5 |
| everolimus |
mTOR inhibitor |
PIK3CA activating mutation, ALK fusion, ESR1 mutation, KRAS G12C, KRAS G12D, BRAF V600E, EGFR exon 19 deletion / L858R, IDH1/2 mutation |
5 |
| icotinib |
EGFR TKI (1st generation) |
EGFR exon 19 deletion / L858R |
5 |
| midostaurin Approved |
FLT3 inhibitor |
FLT3 mutation (ITD/TKD), NPM1 mutation |
5 |
| pralsetinib Approved |
RET inhibitor |
RET fusion or mutation, BRAF V600E, NTRK1/2/3 fusion, ALK fusion, KRAS G12C, ROS1 fusion, EGFR exon 20 insertion |
5 |
| repotrectinib Approved |
ROS1/TRK TKI (next generation) |
ROS1 fusion, NTRK1/2/3 fusion, ALK fusion, EGFR exon 19 deletion / L858R, KRAS G12C, KRAS G12D |
5 |
| safusidenib |
IDH1 inhibitor |
IDH1/2 mutation |
5 |
| tepotinib Approved |
MET TKI |
MET exon 14 skipping, EGFR exon 19 deletion / L858R, ALK fusion |
5 |
| tovorafenib Approved |
pan-RAF inhibitor |
BRAF V600E, FGFR2 fusion or rearrangement, FGFR3 alteration (mutation or fusion), KRAS G12C, KRAS G12D |
5 |
| zipalertinib |
EGFR exon 20 insertion TKI |
EGFR exon 20 insertion, EGFR exon 19 deletion / L858R |
5 |
| bleximenib |
menin inhibitor |
NPM1 mutation |
4 |
| ceralasertib |
ATR inhibitor |
BRCA1/2 mutation, IDH1/2 mutation |
4 |
| DZD6008 |
EGFR TKI (brain-penetrant) |
EGFR exon 19 deletion / L858R |
4 |
| elironrasib |
KRAS G12C inhibitor (ON state) |
KRAS G12C, KRAS G12D |
4 |
| fluzoparib |
PARP inhibitor |
BRCA1/2 mutation, BRAF V600E |
4 |
| GFH276 |
RAS inhibitor |
KRAS G12D, KRAS G12C |
4 |
| HSK42360 |
BRAF inhibitor (paradox breaker, brain-penetrant) |
BRAF V600E |
4 |
| olomorasib |
KRAS G12C inhibitor (ON/OFF) |
KRAS G12C |
4 |
| saruparib |
PARP1-selective inhibitor |
BRCA1/2 mutation |
4 |
| setidegrasib |
KRAS G12D degrader |
KRAS G12D |
4 |
| taletrectinib Approved |
ROS1 TKI (next generation) |
ROS1 fusion, NTRK1/2/3 fusion |
4 |
| veliparib |
PARP inhibitor |
BRCA1/2 mutation, IDH1/2 mutation, EGFR exon 19 deletion / L858R, MSI-H / dMMR |
4 |
| WSD0922 |
EGFR TKI (brain-penetrant) |
EGFR exon 19 deletion / L858R |
4 |
| BBO-10203 |
RAS:PI3Kα interaction blocker |
KRAS G12C, KRAS G12D, PIK3CA activating mutation |
3 |
| capmatinib Approved |
MET TKI |
EGFR exon 19 deletion / L858R, MET exon 14 skipping, ALK fusion, BRAF V600E, ROS1 fusion |
3 |
| ceritinib Approved |
ALK TKI (2nd generation) |
ALK fusion, ROS1 fusion |
3 |
| copanlisib |
PI3K inhibitor |
PIK3CA activating mutation, MSI-H / dMMR, BRAF V600E, BRCA1/2 mutation |
3 |
| deulorlatinib |
ALK/ROS1 TKI (3rd generation) |
ALK fusion, ROS1 fusion |
3 |
| glumetinib |
MET TKI |
EGFR exon 19 deletion / L858R, MET exon 14 skipping |
3 |
| HRS-7058 |
KRAS G12C inhibitor |
KRAS G12C |
3 |
| ipatasertib |
AKT inhibitor |
BRCA1/2 mutation, HER2 (ERBB2) activating mutation, MSI-H / dMMR, PIK3CA activating mutation, ALK fusion, BRAF V600E, RET fusion or mutation |
3 |
| iruplinalkib |
ALK TKI (2nd generation) |
ALK fusion, ROS1 fusion |
3 |
| JYP0322 |
ROS1 TKI |
ROS1 fusion |
3 |
| MCLA-129 |
EGFR-MET bispecific antibody |
EGFR exon 19 deletion / L858R, EGFR exon 20 insertion, MET exon 14 skipping |
3 |
| navitoclax |
BCL-2/BCL-xL inhibitor |
BRAF V600E, BRCA1/2 mutation, KRAS G12C, KRAS G12D, EGFR exon 19 deletion / L858R |
3 |
| NXP900 |
YES1/SRC inhibitor |
ALK fusion, EGFR exon 19 deletion / L858R, IDH1/2 mutation |
3 |
| opnurasib |
KRAS G12C inhibitor (OFF state) |
KRAS G12C |
3 |
| paxalisib |
PI3K/mTOR inhibitor |
BRAF V600E, KRAS G12C, PIK3CA activating mutation |
3 |
| sevabertinib Approved |
HER2 TKI |
HER2 (ERBB2) activating mutation |
3 |
| silevertinib |
EGFR TKI (4th generation) |
EGFR exon 19 deletion / L858R |
3 |
| TY-9591 |
EGFR TKI (deuterated osimertinib) |
EGFR exon 19 deletion / L858R |
3 |
| ZEN-3694 |
BET bromodomain inhibitor |
BRAF V600E, KRAS G12C, KRAS G12D, BRCA1/2 mutation |
3 |
| APG-2449 |
FAK/ALK/ROS1 inhibitor |
ALK fusion, ROS1 fusion |
2 |
| BI 1701963 |
SOS1 inhibitor |
KRAS G12C, KRAS G12D |
2 |
| claturafenib |
BRAF inhibitor (brain-penetrant) |
BRAF V600E |
2 |
| fexagratinib |
FGFR inhibitor |
FGFR2 fusion or rearrangement, FGFR3 alteration (mutation or fusion), MSI-H / dMMR |
2 |
| futibatinib Approved |
FGFR inhibitor (irreversible) |
FGFR2 fusion or rearrangement, KRAS G12C, KRAS G12D, FGFR3 alteration (mutation or fusion) |
2 |
| HMBD-001 |
anti-HER3 antibody |
NRG1 fusion |
2 |
| HMPL-306 |
IDH1/2 inhibitor |
IDH1/2 mutation |
2 |
| imatinib |
BCR-ABL/KIT TKI |
ALK fusion, BRAF V600E, BRCA1/2 mutation, EGFR exon 19 deletion / L858R, KRAS G12D, ROS1 fusion |
2 |
| INCB161734 |
KRAS G12D inhibitor |
KRAS G12D |
2 |
| JMT101 |
anti-EGFR antibody |
EGFR exon 19 deletion / L858R, EGFR exon 20 insertion |
2 |
| luvometinib |
MEK inhibitor |
BRAF V600E, KRAS G12C, KRAS G12D |
2 |
| LY3410738 |
IDH1/2 inhibitor |
IDH1/2 mutation |
2 |
| mirdametinib |
MEK inhibitor |
BRAF V600E, FGFR2 fusion or rearrangement, FGFR3 alteration (mutation or fusion), KRAS G12C, KRAS G12D |
2 |
| mobocertinib |
EGFR exon 20 insertion TKI |
EGFR exon 20 insertion, EGFR exon 19 deletion / L858R, HER2 (ERBB2) activating mutation |
2 |
| naporafenib |
pan-RAF inhibitor |
BRAF V600E, EGFR exon 19 deletion / L858R, KRAS G12C, KRAS G12D |
2 |
| necitumumab |
anti-EGFR antibody |
EGFR exon 19 deletion / L858R, EGFR exon 20 insertion, ALK fusion |
2 |
| neladalkib |
ALK TKI (brain-penetrant, 4th generation) |
ALK fusion |
2 |
| neratinib |
HER2 TKI |
HER2 (ERBB2) activating mutation, EGFR exon 19 deletion / L858R, KRAS G12C, KRAS G12D |
2 |
| ORIC-114 |
brain-penetrant EGFR/HER2 inhibitor |
EGFR exon 20 insertion, EGFR exon 19 deletion / L858R, HER2 (ERBB2) activating mutation |
2 |
| plixorafenib |
BRAF dimer breaker |
BRAF V600E |
2 |
| sitneprotafib |
SHP2 inhibitor |
KRAS G12C |
2 |
| tinengotinib |
multi-kinase inhibitor (FGFR) |
FGFR2 fusion or rearrangement, FGFR3 alteration (mutation or fusion) |
2 |
| TYRA-300 |
FGFR3-selective inhibitor |
FGFR3 alteration (mutation or fusion) |
2 |
| ulixertinib |
ERK inhibitor |
BRAF V600E, KRAS G12C, KRAS G12D, MSI-H / dMMR |
2 |
| VVD-133214 |
WRN helicase inhibitor |
MSI-H / dMMR |
2 |
| ABSK061 |
FGFR2/3-selective inhibitor |
FGFR2 fusion or rearrangement, FGFR3 alteration (mutation or fusion) |
1 |
| afuresertib |
AKT inhibitor |
PIK3CA activating mutation |
1 |
| atebimetinib |
MEK inhibitor |
BRAF V600E, KRAS G12C, KRAS G12D |
1 |
| AZD9574 |
PARP1-selective inhibitor (brain-penetrant) |
BRCA1/2 mutation, HER2-low / ultralow (IHC 1+ or 2+/ISH-), IDH1/2 mutation |
1 |
| batoprotafib |
SHP2 inhibitor |
KRAS G12C, ALK fusion, BRAF V600E |
1 |
| BBO-8520 |
KRAS G12C inhibitor (ON/OFF) |
KRAS G12C |
1 |
| belvarafenib |
pan-RAF inhibitor |
BRAF V600E, KRAS G12C, KRAS G12D |
1 |
| CFT8919 |
EGFR L858R degrader |
EGFR exon 19 deletion / L858R |
1 |
| derazantinib |
FGFR inhibitor |
FGFR2 fusion or rearrangement, FGFR3 alteration (mutation or fusion) |
1 |
| E7386 |
CBP/β-catenin inhibitor |
MSI-H / dMMR |
1 |
| elzovantinib |
MET inhibitor |
MET exon 14 skipping |
1 |
| enzomenib |
menin inhibitor |
FLT3 mutation (ITD/TKD), NPM1 mutation |
1 |
| gedatolisib |
PI3K/mTOR inhibitor |
BRCA1/2 mutation, BRAF V600E, KRAS G12C, KRAS G12D, PIK3CA activating mutation |
1 |
| gunagratinib |
FGFR inhibitor |
FGFR2 fusion or rearrangement, FGFR3 alteration (mutation or fusion) |
1 |
| HMPL-453 |
FGFR inhibitor |
FGFR2 fusion or rearrangement, FGFR3 alteration (mutation or fusion) |
1 |
| HRO761 |
WRN helicase inhibitor |
MSI-H / dMMR |
1 |
| IDH305 |
IDH1 inhibitor |
IDH1/2 mutation |
1 |
| lapatinib |
HER2 TKI |
BRAF V600E, ALK fusion, BRCA1/2 mutation, EGFR exon 19 deletion / L858R, KRAS G12C, KRAS G12D |
1 |
| lirafugratinib Approved |
FGFR2-selective inhibitor |
FGFR2 fusion or rearrangement |
1 |
| lunbotinib |
RET inhibitor (next generation) |
RET fusion or mutation |
1 |
| nazartinib |
EGFR TKI (3rd generation) |
EGFR exon 19 deletion / L858R |
1 |
| osemitamab |
anti-CLDN18.2 antibody |
Claudin 18.2 expression |
1 |
| pamiparib |
PARP inhibitor |
IDH1/2 mutation, BRCA1/2 mutation, MSI-H / dMMR |
1 |
| RLY-2608 |
mutant-selective PI3Kα inhibitor |
PIK3CA activating mutation |
1 |
| siremadlin |
MDM2 inhibitor |
ALK fusion, BRAF V600E, NTRK1/2/3 fusion, ROS1 fusion, FLT3 mutation (ITD/TKD) |
1 |
| ST316 |
β-catenin antagonist |
BRCA1/2 mutation |
1 |
| STX-478 |
mutant-selective PI3Kα inhibitor |
PIK3CA activating mutation |
1 |
| SY-5007 |
RET inhibitor |
RET fusion or mutation |
1 |
| taselisib |
PI3K inhibitor |
PIK3CA activating mutation, KRAS G12C, KRAS G12D |
1 |
| tasurgratinib |
FGFR inhibitor |
FGFR3 alteration (mutation or fusion), FGFR2 fusion or rearrangement |
1 |
| TSN1611 |
KRAS G12D inhibitor |
KRAS G12D |
1 |
| vandetanib |
multi-kinase inhibitor (RET) |
RET fusion or mutation |
1 |
| vociprotafib |
SHP2 inhibitor |
KRAS G12C, EGFR exon 19 deletion / L858R, KRAS G12D |
1 |
| zanidatamab |
HER2 bispecific antibody |
MSI-H / dMMR, HER2-low / ultralow (IHC 1+ or 2+/ISH-) |
1 |
| zenocutuzumab Approved |
HER2/HER3 bispecific antibody |
NRG1 fusion, HER2-low / ultralow (IHC 1+ or 2+/ISH-) |
1 |
| zidesamtinib Approved |
ROS1 TKI (brain-penetrant) |
ROS1 fusion |
1 |
| bemarituzumab |
anti-FGFR2b antibody |
MSI-H / dMMR |
0 |
| berzosertib |
ATR inhibitor |
BRCA1/2 mutation |
0 |
| BLU-451 |
EGFR inhibitor |
EGFR exon 19 deletion / L858R, EGFR exon 20 insertion |
0 |
| buparlisib |
pan-PI3K inhibitor |
BRAF V600E, EGFR exon 19 deletion / L858R, PIK3CA activating mutation |
0 |
| camonsertib |
ATR inhibitor |
KRAS G12C, KRAS G12D |
0 |
| crenolanib |
FLT3 inhibitor |
FLT3 mutation (ITD/TKD) |
0 |
| dactolisib |
PI3K/mTOR inhibitor |
PIK3CA activating mutation |
0 |
| enbezotinib |
RET inhibitor |
RET fusion or mutation |
0 |
| infigratinib |
FGFR inhibitor |
BRAF V600E, FGFR2 fusion or rearrangement, FGFR3 alteration (mutation or fusion), PIK3CA activating mutation |
0 |
| MK-2206 |
AKT inhibitor |
BRAF V600E, EGFR exon 19 deletion / L858R, PIK3CA activating mutation |
0 |
| MRTX1133 |
KRAS G12D inhibitor |
KRAS G12D |
0 |
| ponatinib |
BCR-ABL1 inhibitor |
ALK fusion, FGFR2 fusion or rearrangement, FGFR3 alteration (mutation or fusion), FLT3 mutation (ITD/TKD), KRAS G12C, KRAS G12D, RET fusion or mutation |
0 |
| poziotinib |
EGFR/HER2 inhibitor |
EGFR exon 19 deletion / L858R, EGFR exon 20 insertion, HER2 (ERBB2) activating mutation |
0 |
| rezivertinib |
EGFR TKI (3rd generation) |
EGFR exon 19 deletion / L858R, EGFR exon 20 insertion |
0 |
| rociletinib |
EGFR TKI (3rd generation) |
EGFR exon 19 deletion / L858R, EGFR exon 20 insertion |
0 |
| rogaratinib |
FGFR inhibitor |
FGFR2 fusion or rearrangement, FGFR3 alteration (mutation or fusion) |
0 |
| rucaparib Approved |
PARP inhibitor |
BRCA1/2 mutation |
0 |
| selitrectinib |
TRK inhibitor (next generation) |
NTRK1/2/3 fusion |
0 |
| senaparib |
PARP inhibitor |
BRCA1/2 mutation |
0 |
| serabelisib |
PI3Kα inhibitor |
KRAS G12C, KRAS G12D, PIK3CA activating mutation |
0 |
| seribantumab |
anti-HER3 antibody |
NRG1 fusion |
0 |
| tarloxotinib |
pan-HER prodrug |
EGFR exon 19 deletion / L858R, EGFR exon 20 insertion, HER2 (ERBB2) activating mutation, KRAS G12C, NRG1 fusion |
0 |