Larotrectinib
Sign in to save this workspacePrimary targets: TRKA, TRKB, TRKC · FDA status: FDA Approved
Selectivity scorecard
KISS
99.25
Gini
0.710
CATDS
0.047
Computed from wild-type kinome inhibition at 1 μM. Gini reproduces the published values within tolerance; KISS and CATDS are computed but pending reconciliation with the paper's reference code.
Polypharmacology radar
Top 20 strongest-inhibited wild-type kinases for Larotrectinib. Strongest target: TRKA at 98.5% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | TRKA | 98.5% | 1.5% |
| 2 | TRKC | 98.1% | 1.9% |
| 3 | TRKB | 97.9% | 2.1% |
| 4 | ROS_ROS1 | 89.5% | 10.5% |
| 5 | ACK1 | 57.8% | 42.2% |
| 6 | MUSK | 52.5% | 47.5% |
| 7 | DDR1 | 51.2% | 48.8% |
| 8 | DDR2 | 43.7% | 56.3% |
| 9 | LIMK1 | 32.8% | 67.2% |
| 10 | TXK | 29.6% | 70.4% |
| 11 | ARK5_NUAK1 | 25.7% | 74.3% |
| 12 | BMX_ETK | 25.3% | 74.7% |
| 13 | TYK1_LTK | 20.5% | 79.5% |
| 14 | JAK2 | 20.3% | 79.7% |
| 15 | GRK6 | 19.2% | 80.8% |
| 16 | MST3_STK24 | 19.0% | 81.0% |
| 17 | MLCK2_MYLK2 | 18.7% | 81.3% |
| 18 | CK2A2 | 18.6% | 81.4% |
| 19 | C_MET | 17.4% | 82.6% |
| 20 | PDK2_PDHK2 | 16.7% | 83.3% |
Selectivity landscape
Where Larotrectinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Larotrectinib.
Atlas insights for Larotrectinib
Pathway-space view of what this drug actually does, drawn from the Pathway Atlas.
On-target vs off-target shadow
On-target0%
Off-target100%
Ghost (2nd-order)0%
| Pathway | Composition | Total |Π| |
|---|---|---|
| ADIPOGENESIS | 433.25 | |
| ALLOGRAFT_REJECTION | 1098.03 | |
| ANDROGEN_RESPONSE | 332.96 | |
| ANGIOGENESIS | 197.44 | |
| APICAL_JUNCTION | 1228.55 | |
| APICAL_SURFACE | 156.34 | |
| APOPTOSIS | 1230.82 | |
| BILE_ACID_METABOLISM | 153.00 | |
| CHOLESTEROL_HOMEOSTASIS | 248.57 | |
| COAGULATION | 193.07 | |
| COMPLEMENT | 856.46 | |
| DNA_REPAIR | 303.53 | |
| E2F_TARGETS | 914.29 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 354.32 | |
| ESTROGEN_RESPONSE_EARLY | 574.46 | |
| ESTROGEN_RESPONSE_LATE | 500.04 | |
| FATTY_ACID_METABOLISM | 115.22 | |
| G2M_CHECKPOINT | 903.64 | |
| GLYCOLYSIS | 443.15 | |
| HEDGEHOG_SIGNALING | 149.71 | |
| HEME_METABOLISM | 364.81 | |
| HYPOXIA | 701.62 | |
| IL2_STAT5_SIGNALING | 495.78 | |
| IL6_JAK_STAT3_SIGNALING | 787.81 | |
| INFLAMMATORY_RESPONSE | 740.03 | |
| INTERFERON_ALPHA_RESPONSE | 102.14 | |
| INTERFERON_GAMMA_RESPONSE | 754.58 | |
| KRAS_SIGNALING_DN | 189.19 | |
| KRAS_SIGNALING_UP | 499.82 | |
| MITOTIC_SPINDLE | 1090.22 | |
| MTORC1_SIGNALING | 612.37 | |
| MYC_TARGETS_V1 | 609.93 | |
| MYC_TARGETS_V2 | 123.64 | |
| MYOGENESIS | 541.95 | |
| NOTCH_SIGNALING | 63.78 | |
| OXIDATIVE_PHOSPHORYLATION | 241.65 | |
| P53_PATHWAY | 525.26 | |
| PANCREAS_BETA_CELLS | 49.07 | |
| PEROXISOME | 178.38 | |
| PI3K_AKT_MTOR_SIGNALING | 1409.37 | |
| PROTEIN_SECRETION | 316.76 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 87.69 | |
| SPERMATOGENESIS | 333.29 | |
| TGF_BETA_SIGNALING | 320.19 | |
| TNFA_SIGNALING_VIA_NFKB | 688.39 | |
| UNFOLDED_PROTEIN_RESPONSE | 245.44 | |
| UV_RESPONSE_DN | 750.09 | |
| UV_RESPONSE_UP | 759.90 | |
| WNT_BETA_CATENIN_SIGNALING | 363.67 | |
| XENOBIOTIC_METABOLISM | 270.83 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.863 |
| SRR23303752 | — | 0.849 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.846 |
| SRR12202498 | — | 0.838 |
| TCGA-FD-A43X-01A-11R-A23W-07 | — | 0.833 |
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