Brimapitide, C-Terminal Acid

Summary

Brimapitide, C-Terminal Acid (CHEMBL4297348) is a phase-3 clinical-stage protein targeting MAPK10; indicated across 1 condition including hearing loss disorder.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Protein
• Targets: 1 (MAPK10)
• Indications: 1 condition
• Clinical trials: 3
• Chemistry: 3823.4 Da · C164H285N65O41

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4297348
Name	Brimapitide, C-Terminal Acid
Type	Protein
Max phase	3
FDA approved	no
PubChem CID	72941992
Molecular formula	C164H285N65O41
Molecular weight	3823.4
InChIKey	HRMVIAFZYCCHGF-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)O)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)-5-carbamimidamido-1-(carboxymethylamino)-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: Am-111, AM-111, Brimapitide, c-terminal acid, D-jnki-1, Xg-102 c-terminal acid, BRIMAPITIDE, C-TERMINAL ACID

Patent coverage: 76 distinct patent families (184 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).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
MAPK10	mitogen-activated protein kinase 10	Inhibition	7	0.2%	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:

Pathway	Targets	Genes
Cytokine Signaling in Immune system	1	MAPK10
Toll Like Receptor 4 (TLR4) Cascade	1	MAPK10
MyD88:MAL(TIRAP) cascade initiated on plasma membrane	1	MAPK10
MyD88-independent TLR4 cascade	1	MAPK10
Toll Like Receptor 9 (TLR9) Cascade	1	MAPK10
Toll Like Receptor 10 (TLR10) Cascade	1	MAPK10
Toll Like Receptor 3 (TLR3) Cascade	1	MAPK10
Toll Like Receptor 5 (TLR5) Cascade	1	MAPK10
Toll Like Receptor TLR1:TLR2 Cascade	1	MAPK10
Toll Like Receptor 7/8 (TLR7/8) Cascade	1	MAPK10
Toll Like Receptor TLR6:TLR2 Cascade	1	MAPK10
Innate Immune System	1	MAPK10
Immune System	1	MAPK10
Toll-like Receptor Cascades	1	MAPK10
Toll Like Receptor 2 (TLR2) Cascade	1	MAPK10
Cellular responses to stress	1	MAPK10
Fc epsilon receptor (FCERI) signaling	1	MAPK10
Oxidative Stress Induced Senescence	1	MAPK10
Cellular Senescence	1	MAPK10
FCERI mediated MAPK activation	1	MAPK10
Interleukin-17 signaling	1	MAPK10
Signaling by Interleukins	1	MAPK10
MAPK targets/ Nuclear events mediated by MAP kinases	1	MAPK10
MAP kinase activation	1	MAPK10
JNK (c-Jun kinases) phosphorylation and activation mediated by activated human TAK1	1	MAPK10
Activation of the AP-1 family of transcription factors	1	MAPK10
Cellular responses to stimuli	1	MAPK10
TRIF (TICAM1)-mediated TLR4 signaling	1	MAPK10
TRAF6 mediated induction of NFkB and MAP kinases upon TLR7/8 or 9 activation	1	MAPK10
MyD88 dependent cascade initiated on endosome	1	MAPK10

Dominant GO biological processes

GO term	Targets
protein phosphorylation	1
signal transduction	1
JNK cascade	1
response to light stimulus	1
Fc-epsilon receptor signaling pathway	1
regulation of circadian rhythm	1
rhythmic process	1
cellular senescence	1
MAPK cascade	1
cellular response to stress	1

Indications & clinical

Indications

1 indication (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
hearing loss disorder	3	MONDO:0005365	EFO:0004238

Clinical trials

Total trials: 3.

Phase distribution

Phase	Trials
PHASE3	2
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02561091	PHASE3	COMPLETED	AM-111 in the Treatment of Acute Inner Ear Hearing Loss
NCT02809118	PHASE3	TERMINATED	Efficacy and Safety of AM-111 as Acute Sudden Sensorineural Hearing Loss Treatment
NCT00802425	PHASE2	COMPLETED	Efficacy of AM-111 in Patients With Acute Sensorineural Hearing Loss

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

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:

Molecule	Source	Status	Shared targets
AFATINIB	ChEMBL + PubChem	Phase 4 (approved)	MAPK10
GEFITINIB	ChEMBL + PubChem	Phase 4 (approved)	MAPK10
PAZOPANIB	ChEMBL + PubChem	Phase 4 (approved)	MAPK10
ABEMACICLIB	ChEMBL	Phase 4 (approved)	MAPK10
AXITINIB	ChEMBL	Phase 4 (approved)	MAPK10
ERLOTINIB	ChEMBL	Phase 4 (approved)	MAPK10
FEDRATINIB	ChEMBL	Phase 4 (approved)	MAPK10
FILGOTINIB	ChEMBL	Phase 4 (approved)	MAPK10
GILTERITINIB	ChEMBL	Phase 4 (approved)	MAPK10
IMATINIB	ChEMBL	Phase 4 (approved)	MAPK10
MIDOSTAURIN	ChEMBL	Phase 4 (approved)	MAPK10
MOMELOTINIB	ChEMBL	Phase 4 (approved)	MAPK10
NERATINIB	ChEMBL	Phase 4 (approved)	MAPK10
NILOTINIB	ChEMBL	Phase 4 (approved)	MAPK10
NINTEDANIB	ChEMBL	Phase 4 (approved)	MAPK10
SUNITINIB	ChEMBL	Phase 4 (approved)	MAPK10
ALVOCIDIB	ChEMBL	Phase 3	MAPK10
CANERTINIB	ChEMBL	Phase 3	MAPK10
DOVITINIB	ChEMBL	Phase 3	MAPK10
LESTAURTINIB	ChEMBL	Phase 3	MAPK10
LINIFANIB	ChEMBL	Phase 3	MAPK10
AT-9283	ChEMBL	Phase 2	MAPK10
BAY-1161909	ChEMBL	Phase 2	MAPK10
BENTAMAPIMOD	ChEMBL	Phase 2	MAPK10
BI-2536	ChEMBL	Phase 2	MAPK10
CC-401	ChEMBL	Phase 2	MAPK10
CC-90001	ChEMBL	Phase 2	MAPK10
CEP-32496	ChEMBL	Phase 2	MAPK10
CERDULATINIB	ChEMBL	Phase 2	MAPK10
DORAMAPIMOD	ChEMBL	Phase 2	MAPK10
FORETINIB	ChEMBL	Phase 2	MAPK10
MILCICLIB	ChEMBL	Phase 2	MAPK10
MK-2461	ChEMBL	Phase 2	MAPK10
OSI-027	ChEMBL	Phase 2	MAPK10
PAMAPIMOD	ChEMBL	Phase 2	MAPK10
PEXMETINIB	ChEMBL	Phase 2	MAPK10
PICTILISIB	ChEMBL	Phase 2	MAPK10
R-406	ChEMBL	Phase 2	MAPK10
REBASTINIB	ChEMBL	Phase 2	MAPK10
REFAMETINIB	ChEMBL	Phase 2	MAPK10
SU-014813	ChEMBL	Phase 2	MAPK10
TANZISERTIB	ChEMBL	Phase 2	MAPK10
TOZASERTIB	ChEMBL	Phase 2	MAPK10
VX-702	ChEMBL	Phase 2	MAPK10
Binimetinib	PubChem	Approved	MAPK10
Crizotinib	PubChem	Approved	MAPK10
dacomitinib	PubChem	Approved	MAPK10
Fostamatinib	PubChem	Approved	MAPK10
Idelalisib	PubChem	Approved	MAPK10
podofilox	PubChem	Approved	MAPK10
regorafenib	PubChem	Approved	MAPK10
Selumetinib	PubChem	Approved	MAPK10
Trametinib	PubChem	Approved	MAPK10