Paltusotine

Summary

Paltusotine (CHEMBL5267842) is a phase-3 clinical-stage small molecule targeting SSTR2; indicated across 3 conditions including acromegaly and carcinoid syndrome.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (SSTR2)
• Indications: 3 conditions
• Clinical trials: 9
• Chemistry: 456.5 Da · C27H22F2N4O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL5267842
Name	Paltusotine
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	134168328
Molecular formula	C27H22F2N4O
Molecular weight	456.5
InChIKey	GHILNKWBALQPDP-UHFFFAOYSA-N

SMILES: C1CN(CCC1N)C2=C3C=C(C=CC3=NC=C2C4=CC(=CC(=C4)F)F)C5=CC=CC(=C5O)C#N

IUPAC name: 3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorophenyl)quinolin-6-yl]-2-hydroxybenzonitrile

Also known as: CRN-00808, Crn00808, CRN00808, Paltusotine, PALTUSOTINE

Parent form; salt/anhydrous children: CHEMBL5314560

Patent coverage: 25 distinct patent families (87 SureChEMBL compound mentions), from 3 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
SSTR2	SST2 receptor	Agonist	9.6	0.7%	P30874

Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: Somatostatin receptor type 2, Somatostatin receptor type 4, Somatostatin receptor type 2, Cytochrome P450 2C9, Cytochrome P450 2C19, Somatostatin receptor type 2.

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
SSTR2	9.6	EC50	0.25	nM	CHEMBL_ACT_24979691
SSTR2	9.6	EC50	0.25	nM	CHEMBL_ACT_24979721
P30680	8.92	EC50	1.2	nM	CHEMBL_ACT_24979850
Q49LX6	8.18	EC50	6.6	nM	CHEMBL_ACT_24979851
SSTR4	6	EC50	1000	nM	CHEMBL_ACT_24979753
CYP2C19	5.3	IC50	5012	nM	CHEMBL_ACT_24979816
CYP2C9	5.1	IC50	7943	nM	CHEMBL_ACT_24979814

Target pathways

Aggregated over 1 target gene(s): SSTR2.

Top Reactome pathways

7 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	1	SSTR2
Signaling by GPCR	1	SSTR2
Class A/1 (Rhodopsin-like receptors)	1	SSTR2
Peptide ligand-binding receptors	1	SSTR2
GPCR downstream signalling	1	SSTR2
G alpha (i) signalling events	1	SSTR2
GPCR ligand binding	1	SSTR2

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	1
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	1
neuropeptide signaling pathway	1
negative regulation of cell population proliferation	1
cellular response to glucocorticoid stimulus	1
cellular response to estradiol stimulus	1
signal transduction	1
G protein-coupled receptor signaling pathway	1
somatostatin signaling pathway	1

Indications & clinical

Indications

3 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
acromegaly	3	MONDO:0019933	EFO:1001485
carcinoid syndrome	1	MONDO:0100347	EFO:1000852
neuroendocrine neoplasm	1	MONDO:0019496	EFO:1001901

Clinical trials

Total trials: 9.

Phase distribution

Phase	Trials
PHASE2	4
PHASE3	3
PHASE1	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04837040	PHASE3	ACTIVE_NOT_RECRUITING	A Study to Evaluate the Safety and Efficacy of Paltusotine for the Treatment of Acromegaly
NCT05192382	PHASE3	ACTIVE_NOT_RECRUITING	A Study to Evaluate the Safety and Efficacy of Paltusotine for the Treatment of Acromegaly (PATHFNDR-2)
NCT07087054	PHASE3	RECRUITING	Carcinoid Syndrome Efficacy Study Featuring an Oral Daily Paltusotine Regimen
NCT04261712	PHASE2	ACTIVE_NOT_RECRUITING	A Study to Evaluate the Long-Term Safety and Efficacy of Paltusotine for the Treatment of Acromegaly (ACROBAT Advance)
NCT03789656	PHASE2	COMPLETED	An Study to Evaluate the Safety and Efficacy of Paltusotine for the Treatment of Acromegaly (ACROBAT Edge)
NCT03792555	PHASE2	COMPLETED	A Study to Evaluate the Safety and Efficacy of Paltusotine for the Treatment of Acromegaly (ACROBAT Evolve)
NCT05361668	PHASE2	COMPLETED	Study to Evaluate the Safety, PK, and Dose Response of Paltusotine in Subjects With Carcinoid Syndrome
NCT03276858	PHASE1	COMPLETED	Single and Multiple-Ascending Dose Study of CRN00808 in Healthy Volunteers
NCT04246749	PHASE1	COMPLETED	Mass Balance and Pharmacokinetics of [14C]-CRN00808 in 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.

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.

11 molecules share ≥1 primary target. Top 11 by shared-target count:

Molecule	Source	Status	Shared targets
GALLIUM OXODOTREOTIDE	ChEMBL	Phase 4 (approved)	SSTR2
LANREOTIDE	ChEMBL	Phase 4 (approved)	SSTR2
OCTREOTIDE	ChEMBL	Phase 4 (approved)	SSTR2
PASIREOTIDE	ChEMBL	Phase 4 (approved)	SSTR2
EDOTREOTIDE	ChEMBL	Phase 3	SSTR2
SOMATOSTATIN	ChEMBL	Phase 3	SSTR2
VAPREOTIDE	ChEMBL	Phase 3	SSTR2
EDOTREOTIDE YTTRIUM	ChEMBL	Phase 2	SSTR2
MK-8189	ChEMBL	Phase 2	SSTR2
SEGLITIDE	ChEMBL	Phase 2	SSTR2
oxodotreotide	PubChem	Approved	SSTR2