Florbetapir

Summary

Florbetapir (CHEMBL1908919) is an approved small molecule.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Clinical trials: 8
• Chemistry: 360.4 Da · C20H25FN2O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1908919
Name	Florbetapir
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	57396865
Molecular formula	C20H25FN2O3
Molecular weight	360.4
InChIKey	YNDIAUKFXKEXSV-NSCUHMNNSA-N

SMILES: CNC1=CC=C(C=C1)/C=C/C2=CN=C(C=C2)OCCOCCOCCF

IUPAC name: 4-[(E)-2-[6-[2-[2-(2-fluoroethoxy)ethoxy]ethoxy]-3-pyridinyl]ethenyl]-N-methylaniline

Also known as: Av-45, Florbetapir, FLORBETAPIR, FLORPIRAMINE F 18

Parent form; salt/anhydrous children: CHEMBL1774461

Patent coverage: 319 distinct patent families (690 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 591 (86%) 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: 3 (assay-derived). Sample: Microtubule-associated protein tau, Amyloid-beta precursor protein, Alpha-synuclein.

Bioactivity

ChEMBL activities: 7 potent at pChembl ≥ 5 of 7 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
APP	7.94	Ki	11.4	nM	CHEMBL_ACT_16453375
APP	7.89	Ki	12.8	nM	CHEMBL_ACT_13387456
MAPT	7.71	Kd	19.6	nM	CHEMBL_ACT_28237994
SNCA	7.61	Kd	24.3	nM	CHEMBL_ACT_28237931
SNCA	7.61	Kd	24.3	nM	CHEMBL_ACT_28237997
MAPT	7.51	Ki	30.6	nM	CHEMBL_ACT_28237862
SNCA	7.12	Ki	76.6	nM	CHEMBL_ACT_28237859

Target pathways

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

Indications & clinical

Indications

0 indications (0 at ChEMBL trial phase 4).

Clinical trials

Total trials: 8.

Phase distribution

Phase	Trials
PHASE2	3
PHASE4	2
Not specified	2
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01946243	PHASE4	COMPLETED	The Feasibility of Florbetapir Quantitation
NCT03040427	PHASE4	TERMINATED	The Role of F-18 Florbetapir in the Early Detection of Cardiac Amyloidosis
NCT02813434	PHASE3	UNKNOWN	Cerebral Amyloid Imaging Using Florbetapir (AV-45)
NCT01890343	PHASE2	COMPLETED	Imaging Characteristics of Florbetapir 18F in Patients With Frontotemporal Dementia, Alzheimer’s Disease and Normal Controls.
NCT02667496	PHASE2	WITHDRAWN	Safety Study of Sargramostim in Treating Patients With Mild Cognitive Impairment Due to Alzheimer’s Disease
NCT04588649	PHASE2	COMPLETED	The Aging Brain and Cognition: Contribution of Vascular Injury, Amyloid Plaque and Tau Protein to Cognitive Dysfunction After Stroke
NCT01231971	Not specified	COMPLETED	Alzheimer’s Disease Neuroimaging Initiative 2
NCT02759887	Not specified	COMPLETED	Relationship Between Down Syndrome (DS) and Alzheimer’s Disease (AD)

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

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