Tinlarebant

Summary

Tinlarebant (CHEMBL3967849) is a phase-3 clinical-stage small molecule targeting RBP4; indicated across 4 conditions including stargardt disease and age-related macular degeneration.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (RBP4)
• Indications: 4 conditions
• Clinical trials: 7
• Chemistry: 456.4 Da · C21H21F5N4O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3967849
Name	Tinlarebant
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	92044505
Molecular formula	C21H21F5N4O2
Molecular weight	456.4
InChIKey	HAGSLCBZFRRBLS-UHFFFAOYSA-N

SMILES: CC(=O)N1CCC2=C(C1)NN=C2C(=O)N3CCC(CC3)C4=C(C(=C(C=C4)F)F)C(F)(F)F

IUPAC name: 1-[3-[4-[3,4-difluoro-2-(trifluoromethyl)phenyl]piperidine-1-carbonyl]-1,4,5,7-tetrahydropyrazolo[5,4-c]pyridin-6-yl]ethanone

Also known as: Bpn-14967, BPN-14967, Lbs-008, LBS-008, Tinlarebant, TINLAREBANT

Patent coverage: 15 distinct patent families (64 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
RBP4	retinol binding protein 4	Inhibition	8.35	0.2%	P02753

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Retinol-binding protein 4.

Bioactivity

ChEMBL activities: 38 potent at pChembl ≥ 5 of 38 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
RBP4	8.55	IC50	2.82	nM	CHEMBL_ACT_17795236
RBP4	8.36	IC50	4.33	nM	CHEMBL_ACT_17795237
RBP4	8.36	IC50	4.33	nM	CHEMBL_ACT_26879931
RBP4	8.36	IC50	4.33	nM	CHEMBL_ACT_26879937
RBP4	8.36	IC50	4.33	nM	CHEMBL_ACT_26879940
RBP4	8.36	IC50	4.33	nM	CHEMBL_ACT_27318602
RBP4	8.36	IC50	4.33	nM	CHEMBL_ACT_27318605
RBP4	8.36	IC50	4.33	nM	CHEMBL_ACT_27318608
RBP4	8.36	IC50	4.33	nM	CHEMBL_ACT_27740216
RBP4	8.36	IC50	4.33	nM	CHEMBL_ACT_27740219
RBP4	8.36	IC50	4.33	nM	CHEMBL_ACT_27740222
RBP4	8.36	IC50	4.33	nM	CHEMBL_ACT_28242956
RBP4	8.36	IC50	4.33	nM	CHEMBL_ACT_28242959
RBP4	8.36	IC50	4.33	nM	CHEMBL_ACT_28242962
RBP4	8.36	IC50	4.33	nM	CHEMBL_ACT_29004500
RBP4	8.36	IC50	4.33	nM	CHEMBL_ACT_29004506
RBP4	8.36	IC50	4.33	nM	CHEMBL_ACT_29004509
RBP4	8.28	IC50	5.26	nM	CHEMBL_ACT_17795235
RBP4	8.22	IC50	6.04	nM	CHEMBL_ACT_17795234
RBP4	8.22	IC50	6.04	nM	CHEMBL_ACT_26879925
RBP4	8.22	IC50	6.04	nM	CHEMBL_ACT_27318599
RBP4	8.22	IC50	6.04	nM	CHEMBL_ACT_27740213
RBP4	8.22	IC50	6.04	nM	CHEMBL_ACT_28242953
RBP4	8.22	IC50	6.04	nM	CHEMBL_ACT_29004494
RBP4	8.04	IC50	9.12	nM	CHEMBL_ACT_17795233
RBP4	8.04	IC50	9.12	nM	CHEMBL_ACT_26879919
RBP4	8.04	IC50	9.12	nM	CHEMBL_ACT_27318596
RBP4	8.04	IC50	9.12	nM	CHEMBL_ACT_27740210
RBP4	8.04	IC50	9.12	nM	CHEMBL_ACT_28242950
RBP4	8.04	IC50	9.12	nM	CHEMBL_ACT_29004488

Target pathways

Aggregated over 1 target gene(s): RBP4.

Top Reactome pathways

4 total, by targets touching each:

Pathway	Targets	Genes
The canonical retinoid cycle in rods (twilight vision)	1	RBP4
Retinoid metabolism disease events	1	RBP4
Retinoid metabolism and transport	1	RBP4
Defective visual phototransduction due to STRA6 loss of function	1	RBP4

Dominant GO biological processes

GO term	Targets
eye development	1
positive regulation of immunoglobulin production	1
gluconeogenesis	1
spermatogenesis	1
heart development	1
phototransduction, visible light	1
male gonad development	1
response to xenobiotic stimulus	1
response to muscle activity	1
maintenance of gastrointestinal epithelium	1
lung development	1
positive regulation of insulin secretion	1
response to retinoic acid	1
response to insulin	1
retinol transport	1

Indications & clinical

Indications

4 indications (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
Stargardt disease	3	MONDO:0019353	MONDO:0019353
age-related macular degeneration	1	MONDO:0005150	EFO:0001365
wet macular degeneration	1	MONDO:0005417	EFO:0004683

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 7.

Phase distribution

Phase	Trials
PHASE1	3
PHASE3	2
PHASE2/PHASE3	1
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05949593	PHASE3	ACTIVE_NOT_RECRUITING	Phase 3, Randomized, Placebo-Controlled Study of Tinlarebant to Explore Safety and Efficacy in Geographic Atrophy
NCT06388083	PHASE2/PHASE3	ACTIVE_NOT_RECRUITING	A Phase 2/3 Study to Evaluate the Efficacy and Safety of Tinlarebant in Subjects With Stargardt Disease
NCT05244304	PHASE3	COMPLETED	Phase 3, Randomized, Placebo-Controlled Study of Tinlarebant to Explore Safety and Efficacy in Adolescent Stargardt Disease
NCT05266014	PHASE1/PHASE2	COMPLETED	This is a Dose-finding Study Followed by 2-year Extension Study to Evaluate Safety and Tolerability of Tinlarebant in Adolescent Subjects With Stargardt Disease
NCT03735810	PHASE1	COMPLETED	Safety and Tolerability Study of LBS-008 in Healthy Adult Subjects After Single and Multiple Doses
NCT04005807	PHASE1	COMPLETED	Safety and Tolerability of Escalating Doses of BPN-14967 in Healthy Adults
NCT05667688	PHASE1	COMPLETED	Pharmacokinetics and Pharmacodynamics Study of LBS-008 in Healthy Volunteers Aged 50-85

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

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.

6 molecules share ≥1 primary target. Top 6 by shared-target count:

Molecule	Source	Status	Shared targets
RETINOL	ChEMBL + PubChem	Phase 4 (approved)	RBP4
FENRETINIDE	ChEMBL	Phase 3	RBP4
Acoramidis	PubChem	Approved	RBP4
Doconexent	PubChem	Approved	RBP4
Palmitic Acid	PubChem	Approved	RBP4
Tafamidis	PubChem	Approved	RBP4