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Brimapitide

drug
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Also known as BrimapitidaXg-102

Summary

Brimapitide (CHEMBL4297650) is a phase-3 clinical-stage protein targeting MAPK10; indicated across 1 condition.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Protein
  • Targets: 1 (MAPK10)
  • Indications: 1 condition
  • Clinical trials: 3
  • Chemistry: 3822.4 Da · C164H286N66O40

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL4297650
NameBrimapitide
TypeProtein
Max phase3
FDA approvedno
PubChem CID90479374
Molecular formulaC164H286N66O40
Molecular weight3822.4
InChIKeyBAAXVYBAMNDCIB-BMCUWHFPSA-N

SMILES: C[C@@H]([C@H](C(=O)N[C@H]([C@H](C)O)C(=O)N1CCC[C@@H]1C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(=O)N2CCC[C@@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)N3CCC[C@@H]3C(=O)N4CCC[C@@H]4C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CCC(=O)N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(=O)N[C@H](CCCCN)C(=O)N[C@H](CCCNC(=N)N)C(=O)NCC(=O)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(=O)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC5=CC=CC=C5)NC(=O)[C@H]6CCCN6C(=O)[C@@H](CCC(=O)N)NC(=O)[C@@H](C(C)C)NC(=O)[C@H]7CCCN7C(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CCC(=O)N)NC(=O)[C@@H](CC(=O)O)N)O

IUPAC name: (3R)-3-amino-4-[[(2R)-5-amino-1-[[(2R)-1-[[(2R)-1-[(2R)-2-[[(2R)-1-[[(2R)-5-amino-1-[(2R)-2-[[(2R)-1-[[(2R)-1-[[(2R)-4-amino-1-[[(2R)-1-[[(2R,3S)-1-[[(2R,3S)-1-[(2R)-2-[[(2R)-1-[[(2R)-6-amino-1-[(2R)-2-[[(2R)-1-[(2R)-2-[(2R)-2-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-5-amino-1-[[(2R)-1-[[(2R)-1-[[(2R)-6-amino-1-[[(2R)-6-amino-1-[[(2R)-1-[(2-amino-2-oxoethyl)amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamoyl]pyrrolidin-1-yl]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-oxobutanoic acid

Also known as: Brimapitida, Brimapitide, Xg-102, BRIMAPITIDE

Patent coverage: 58 distinct patent families (143 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
MAPK10mitogen-activated protein kinase 10Inhibition70.2%P53779

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 1 target gene(s): MAPK10.

Top Reactome pathways

31 total, by targets touching each:

PathwayTargetsGenes
Cytokine Signaling in Immune system1MAPK10
Toll Like Receptor 4 (TLR4) Cascade1MAPK10
MyD88:MAL(TIRAP) cascade initiated on plasma membrane1MAPK10
MyD88-independent TLR4 cascade1MAPK10
Toll Like Receptor 9 (TLR9) Cascade1MAPK10
Toll Like Receptor 10 (TLR10) Cascade1MAPK10
Toll Like Receptor 3 (TLR3) Cascade1MAPK10
Toll Like Receptor 5 (TLR5) Cascade1MAPK10
Toll Like Receptor TLR1:TLR2 Cascade1MAPK10
Toll Like Receptor 7/8 (TLR7/8) Cascade1MAPK10
Toll Like Receptor TLR6:TLR2 Cascade1MAPK10
Innate Immune System1MAPK10
Immune System1MAPK10
Toll-like Receptor Cascades1MAPK10
Toll Like Receptor 2 (TLR2) Cascade1MAPK10
Cellular responses to stress1MAPK10
Fc epsilon receptor (FCERI) signaling1MAPK10
Oxidative Stress Induced Senescence1MAPK10
Cellular Senescence1MAPK10
FCERI mediated MAPK activation1MAPK10
Interleukin-17 signaling1MAPK10
Signaling by Interleukins1MAPK10
MAPK targets/ Nuclear events mediated by MAP kinases1MAPK10
MAP kinase activation1MAPK10
JNK (c-Jun kinases) phosphorylation and activation mediated by activated human TAK11MAPK10
Activation of the AP-1 family of transcription factors1MAPK10
Cellular responses to stimuli1MAPK10
TRIF (TICAM1)-mediated TLR4 signaling1MAPK10
TRAF6 mediated induction of NFkB and MAP kinases upon TLR7/8 or 9 activation1MAPK10
MyD88 dependent cascade initiated on endosome1MAPK10

Dominant GO biological processes

GO termTargets
protein phosphorylation1
signal transduction1
JNK cascade1
response to light stimulus1
Fc-epsilon receptor signaling pathway1
regulation of circadian rhythm1
rhythmic process1
cellular senescence1
MAPK cascade1
cellular response to stress1

Indications & clinical

Indications

1 indication (0 at ChEMBL trial phase 4).

The 1 indication record carries no mapped disease name (EFO/MeSH-only); none shown.

Clinical trials

Total trials: 3.

Phase distribution

PhaseTrials
PHASE32
PHASE11

Top trials by phase / activity

NCTPhaseStatusTitle
NCT02235272PHASE3COMPLETEDEfficacy and Safety of XG-102 in Reduction of Post-cataract Surgery Intraocular Inflammation
NCT02508337PHASE3COMPLETEDEfficacy and Safety of XG-102 in Reduction of Post-cataract Surgery Intraocular Inflammation and Pain
NCT01570205PHASE1COMPLETEDSafety, Tolerability and PK of a Single iv Infusion of 10, 40, and 80 µg/kg XG-102 Administered to Healthy Volunteers

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

53 molecules share ≥1 primary target. Top 53 by shared-target count:

MoleculeSourceStatusShared targets
AFATINIBChEMBL + PubChemPhase 4 (approved)MAPK10
GEFITINIBChEMBL + PubChemPhase 4 (approved)MAPK10
PAZOPANIBChEMBL + PubChemPhase 4 (approved)MAPK10
ABEMACICLIBChEMBLPhase 4 (approved)MAPK10
AXITINIBChEMBLPhase 4 (approved)MAPK10
ERLOTINIBChEMBLPhase 4 (approved)MAPK10
FEDRATINIBChEMBLPhase 4 (approved)MAPK10
FILGOTINIBChEMBLPhase 4 (approved)MAPK10
GILTERITINIBChEMBLPhase 4 (approved)MAPK10
IMATINIBChEMBLPhase 4 (approved)MAPK10
MIDOSTAURINChEMBLPhase 4 (approved)MAPK10
MOMELOTINIBChEMBLPhase 4 (approved)MAPK10
NERATINIBChEMBLPhase 4 (approved)MAPK10
NILOTINIBChEMBLPhase 4 (approved)MAPK10
NINTEDANIBChEMBLPhase 4 (approved)MAPK10
SUNITINIBChEMBLPhase 4 (approved)MAPK10
ALVOCIDIBChEMBLPhase 3MAPK10
CANERTINIBChEMBLPhase 3MAPK10
DOVITINIBChEMBLPhase 3MAPK10
LESTAURTINIBChEMBLPhase 3MAPK10
LINIFANIBChEMBLPhase 3MAPK10
AT-9283ChEMBLPhase 2MAPK10
BAY-1161909ChEMBLPhase 2MAPK10
BENTAMAPIMODChEMBLPhase 2MAPK10
BI-2536ChEMBLPhase 2MAPK10
CC-401ChEMBLPhase 2MAPK10
CC-90001ChEMBLPhase 2MAPK10
CEP-32496ChEMBLPhase 2MAPK10
CERDULATINIBChEMBLPhase 2MAPK10
DORAMAPIMODChEMBLPhase 2MAPK10
FORETINIBChEMBLPhase 2MAPK10
MILCICLIBChEMBLPhase 2MAPK10
MK-2461ChEMBLPhase 2MAPK10
OSI-027ChEMBLPhase 2MAPK10
PAMAPIMODChEMBLPhase 2MAPK10
PEXMETINIBChEMBLPhase 2MAPK10
PICTILISIBChEMBLPhase 2MAPK10
R-406ChEMBLPhase 2MAPK10
REBASTINIBChEMBLPhase 2MAPK10
REFAMETINIBChEMBLPhase 2MAPK10
SU-014813ChEMBLPhase 2MAPK10
TANZISERTIBChEMBLPhase 2MAPK10
TOZASERTIBChEMBLPhase 2MAPK10
VX-702ChEMBLPhase 2MAPK10
BinimetinibPubChemApprovedMAPK10
CrizotinibPubChemApprovedMAPK10
dacomitinibPubChemApprovedMAPK10
FostamatinibPubChemApprovedMAPK10
IdelalisibPubChemApprovedMAPK10
podofiloxPubChemApprovedMAPK10
regorafenibPubChemApprovedMAPK10
SelumetinibPubChemApprovedMAPK10
TrametinibPubChemApprovedMAPK10

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot