Zoptarelin Doxorubicin

Summary

Zoptarelin Doxorubicin (CHEMBL3544954) is a phase-3 clinical-stage protein; indicated across 3 conditions including endometrium neoplasm and breast neoplasm.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Protein
• Indications: 3 conditions
• Clinical trials: 4
• Chemistry: 1893 Da · C91H117N19O26

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3544954
Name	Zoptarelin Doxorubicin
Type	Protein
Max phase	3
FDA approved	no
PubChem CID	16158184
Molecular formula	C91H117N19O26
Molecular weight	1893
InChIKey	OOUACICUAVTCEC-LZHWUUGESA-N

SMILES: C[C@H]1[C@H]([C@H](C[C@@H](O1)O[C@H]2C[C@@](CC3=C2C(=C4C(=C3O)C(=O)C5=C(C4=O)C(=CC=C5)OC)O)(C(=O)COC(=O)CCCC(=O)NCCCC[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N6CCC[C@H]6C(=O)NCC(=O)N)NC(=O)[C@H](CC7=CC=C(C=C7)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC8=CNC9=CC=CC=C98)NC(=O)[C@H](CC1=CNC=N1)NC(=O)[C@@H]1CCC(=O)N1)O)N)O

IUPAC name: [2-[(2S,4S)-4-[(2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyloxan-2-yl]oxy-2,5,12-trihydroxy-7-methoxy-6,11-dioxo-3,4-dihydro-1H-tetracen-2-yl]-2-oxoethyl] 5-[[(5R)-6-[[(2S)-1-[[(2S)-1-[(2S)-2-[(2-amino-2-oxoethyl)carbamoyl]pyrrolidin-1-yl]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-[[(2S)-2-[[(2S)-3-hydroxy-2-[[(2S)-2-[[(2S)-3-(1H-imidazol-4-yl)-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-6-oxohexyl]amino]-5-oxopentanoate

Also known as: Aezs-108, AN-152, Zoptarelin doxorubicin, Zoptarelina doxorubicina, Zoptareline doxorubicine, ZOPTARELIN DOXORUBICIN

Parent form; salt/anhydrous children: CHEMBL3989956

Patent coverage: 98 distinct patent families (258 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 256 (99%) 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

No target linkage available.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

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

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
endometrium neoplasm	3	MONDO:0021251	MONDO:0011962
breast neoplasm	2	MONDO:0021100	MONDO:0007254
urothelial carcinoma	1	MONDO:0040679	EFO:0008528

Clinical trials

Total trials: 4.

Phase distribution

Phase	Trials
PHASE2	2
PHASE3	1
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01767155	PHASE3	COMPLETED	Zoptarelin Doxorubicin (AEZS 108) as Second Line Therapy for Endometrial Cancer
NCT00569257	PHASE2	COMPLETED	Antitumoral Activity and Safety of AEZS-108 in Women With LHRH Receptor Positive Gynecological Tumors
NCT01234519	PHASE1/PHASE2	TERMINATED	A Phase I/II Trial of AEZS-108 in Urothelial Cancer Patients Who Failed Platinum-chemotherapy
NCT01698281	PHASE2	TERMINATED	Phase 2 Trial of AEZS-108 in Chemotherapy Refractory in Triple Negative Breast Cancer

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).