Fiboflapon

Summary

Fiboflapon (CHEMBL1922660) is a phase-3 clinical-stage small molecule; indicated across 1 condition including asthma.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 1 condition
• Clinical trials: 9
• Chemistry: 637.8 Da · C38H43N3O4S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1922660
Name	Fiboflapon
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	44473151
Molecular formula	C38H43N3O4S
Molecular weight	637.8
InChIKey	DFQGDHBGRSTTHX-UHFFFAOYSA-N

SMILES: CCOC1=NC=C(C=C1)C2=CC=C(C=C2)CN3C4=C(C=C(C=C4)OCC5=NC=C(C=C5)C)C(=C3CC(C)(C)C(=O)O)SC(C)(C)C

IUPAC name: 3-[3-tert-butylsulfanyl-1-[[4-(6-ethoxy-3-pyridinyl)phenyl]methyl]-5-[(5-methyl-2-pyridinyl)methoxy]indol-2-yl]-2,2-dimethylpropanoic acid

Also known as: AM-803, Am803, Fiboflapon, GSK-2190915, GSK2190915, GSK2190915B, CHEMBL1922660, FIBOFLAPON, AM803, US8772495, 2, Fiboflapon sodium

Parent form; salt/anhydrous children: CHEMBL1922673

Patent coverage: 91 distinct patent families (303 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 194 (64%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 5 (assay-derived). Sample: Leukotriene C4 synthase, Arachidonate 5-lipoxygenase-activating protein, Polyunsaturated fatty acid 5-lipoxygenase, Prostaglandin G/H synthase 1, Arachidonate 5-lipoxygenase-activating protein.

Bioactivity

ChEMBL activities: 11 potent at pChembl ≥ 5 of 14 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ALOX5AP	9.15	IC50	0.7	nM	CHEMBL_ACT_7950109
ALOX5AP	9	IC50	1	nM	CHEMBL_ACT_7950144
ALOX5AP	9	IC50	1	nM	CHEMBL_ACT_7950148
ALOX5AP	8.54	IC50	2.9	nM	CHEMBL_ACT_17637397
ALOX5AP	8.54	IC50	2.9	nM	CHEMBL_ACT_7949342
ALOX5AP	8.4	IC50	4	nM	CHEMBL_ACT_7950156
P20291	7.8	IC50	16	nM	CHEMBL_ACT_7950216
ALOX5AP	7.58	IC50	26	nM	CHEMBL_ACT_7950152
ALOX5AP	7.12	IC50	76	nM	CHEMBL_ACT_7950062
P20291	6.62	IC50	239	nM	CHEMBL_ACT_7950217
ALOX5AP	6.3	IC50	506	nM	CHEMBL_ACT_7949389

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

1 disease in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
asthma	2	MONDO:0004979	MONDO:0004979

Clinical trials

Total trials: 9.

Phase distribution

Phase	Trials
PHASE2	5
PHASE1	4

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00812773	PHASE2	COMPLETED	Study to Evaluate GSK2190915 in Subjects With Mild Asthma
NCT00812929	PHASE2	COMPLETED	A Clinical Trial to Test a Study Drug in Volunteers Who Develop Asthma Following Exercise
NCT01147744	PHASE2	COMPLETED	Dose Ranging Study Evaluating the Efficacy and Safety of GSK2190915 Administered Once Daily
NCT01156792	PHASE2	COMPLETED	Safety and Efficacy Study of Adding GSK2190915 to Low Dose Inhaled Corticosteroid Treatment for Asthma Subjects > or = 12 Years of Age
NCT01471665	PHASE2	COMPLETED	GSK2190915 Neutrophilic Asthma Study
NCT00955383	PHASE1	COMPLETED	GSK2190915 Safety and Pharmacokinetic Study in Healthy Japanese Subjects
NCT01411111	PHASE1	COMPLETED	A Repeat Dose Study to Investigate the Interaction of GSK2190915 on the Pharmacokinetics of Rosuvastatin
NCT01721135	PHASE1	WITHDRAWN	A Study to Evaluate the Effect of Two Different Repeat Doses of GSK2190915 on the QTc Interval.
NCT02224521	PHASE1	COMPLETED	GSK2190915A - Bioavailability Study

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 2 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).