Tiludronic Acid

Summary

Tiludronic Acid (CHEMBL1350) is an approved small molecule (ATC M05BA05) targeting MMP2; indicated across 2 conditions including bone disorder and otosclerosis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: M05BA05
• Targets: 1 (MMP2)
• Indications: 2 conditions
• Clinical trials: 1
• Chemistry: 318.61 Da · C7H9ClO6P2S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1350
Name	Tiludronic Acid
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	60937
ATC	M05BA05
Molecular formula	C7H9ClO6P2S
Molecular weight	318.61
InChIKey	DKJJVAGXPKPDRL-UHFFFAOYSA-N

SMILES: C1=CC(=CC=C1SC(P(=O)(O)O)P(=O)(O)O)Cl

IUPAC name: [(4-chlorophenyl)sulfanyl-phosphonomethyl]phosphonic acid

Also known as: Acide tiludronique, Acido tiludronico, Skelid, SR 41319, SR-41319, Tiludronate, Tiludronic acid, tiludronate, ACIDE_TILUDRONIQUE, TILUDRONIC ACID, Tiludronate disodium

Parent form; salt/anhydrous children: CHEMBL1200448

Patent coverage: 3,605 distinct patent families (14,784 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
MMP2	MMP2	Inhibition	5.14	0.1%	P08253

Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: 72 kDa type IV collagenase, Matrix metalloproteinase-14, Neutrophil collagenase.

Bioactivity

ChEMBL activities: 1 potent at pChembl ≥ 5 of 3 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
MMP2	5.14	IC50	7200	nM	CHEMBL_ACT_13500876

Target pathways

Aggregated over 1 target gene(s): MMP2.

Top Reactome pathways

20 total, by targets touching each:

Pathway	Targets	Genes
Developmental Biology	1	MMP2
Cytokine Signaling in Immune system	1	MMP2
Collagen degradation	1	MMP2
Degradation of the extracellular matrix	1	MMP2
Extracellular matrix organization	1	MMP2
Activation of Matrix Metalloproteinases	1	MMP2
Signal Transduction	1	MMP2
Immune System	1	MMP2
EPH-Ephrin signaling	1	MMP2
Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)	1	MMP2
Metabolism of proteins	1	MMP2
EPH-ephrin mediated repulsion of cells	1	MMP2
Axon guidance	1	MMP2
Signaling by Interleukins	1	MMP2
MAPK6/MAPK4 signaling	1	MMP2
Interleukin-4 and Interleukin-13 signaling	1	MMP2
ESR-mediated signaling	1	MMP2
Signaling by Nuclear Receptors	1	MMP2
Extra-nuclear estrogen signaling	1	MMP2
Nervous system development	1	MMP2

Dominant GO biological processes

GO term	Targets
angiogenesis	1
ovarian follicle development	1
ovulation from ovarian follicle	1
luteinization	1
response to hypoxia	1
blood vessel maturation	1
intramembranous ossification	1
proteolysis	1
negative regulation of cell adhesion	1
heart development	1
parturition	1
response to xenobiotic stimulus	1
response to mechanical stimulus	1
peripheral nervous system axon regeneration	1
response to activity	1

Indications & clinical

Indications

2 indications (1 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
bone disorder	4	MONDO:0005381	EFO:0004260
otosclerosis	3	MONDO:0005349	EFO:0004213

Clinical trials

Total trials: 1.

Phase distribution

Phase	Trials
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01617057	PHASE3	TERMINATED	Therapeutic Efficacy of Tiludronic Acid on Inner Ear Involvement in Advanced Otosclerosis

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 1 clinical and 0 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

23 molecules share ≥1 primary target. Top 23 by shared-target count:

Molecule	Source	Status	Shared targets
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	MMP2
DAUNORUBICIN	ChEMBL	Phase 4 (approved)	MMP2
DOXORUBICIN	ChEMBL	Phase 4 (approved)	MMP2
DOXYCYCLINE	ChEMBL	Phase 4 (approved)	MMP2
ZOLEDRONIC ACID	ChEMBL	Phase 4 (approved)	MMP2
ACLARUBICIN	ChEMBL	Phase 3	MMP2
CAFFEIC ACID	ChEMBL	Phase 3	MMP2
EPIGALOCATECHIN GALLATE	ChEMBL	Phase 3	MMP2
MARIMASTAT	ChEMBL	Phase 3	MMP2
MEDRONIC ACID	ChEMBL	Phase 3	MMP2
PRINOMASTAT	ChEMBL	Phase 3	MMP2
QUERCETIN	ChEMBL	Phase 3	MMP2
ALDUMASTAT	ChEMBL	Phase 2	MMP2
BATIMASTAT	ChEMBL	Phase 2	MMP2
CIPEMASTAT	ChEMBL	Phase 2	MMP2
CTS-1027	ChEMBL	Phase 2	MMP2
ILOMASTAT	ChEMBL	Phase 2	MMP2
LUTEOLIN	ChEMBL	Phase 2	MMP2
REBIMASTAT	ChEMBL	Phase 2	MMP2
SOLIMASTAT	ChEMBL	Phase 2	MMP2
TANOMASTAT	ChEMBL	Phase 2	MMP2
TOSEDOSTAT	ChEMBL	Phase 2	MMP2
UBENIMEX	ChEMBL	Phase 2	MMP2