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MedKoo product information:
Description of AEZS-108: AEZS-108 (AN-152, or
zoptarelin doxorubicin) is a targeted cytotoxic peptide conjugate
which is a hybrid molecule composed of a synthetic peptide carrier
and a well-known cytotoxic agent, doxorubicin. The design of this
product allows for the specific binding and selective uptake of the
cytotoxic conjugate by the LHRH receptor-positive tumors. The
binding of conjugate molecule AEZS-108 to cancerous cells that
express these receptors results in its accumulation in the malignant
tissue. This binding is followed by internalization and retention of
the cytotoxic drug, doxorubicin, in the cells. Therefore, since they
target specific cells, cytotoxic conjugates are postulated to be
more effective and have less side-effects than the respective
non-conjugated/non-linked cytotoxic agents in inhibiting tumor
growth. AEZS-108 is the first drug in a clinical study that targets
the cytotoxic activity of doxorubicin specifically to LHRH-receptor
expressing tumors. (source:
MedKoo Code#: 204220
code name: AEZS-108, AN-152.
Chemical Formula: C91H117N19O26
Exact Mass: 1891.84172
Molecular Weight: 1893.01
Elemental Analysis: C, 57.74; H, 6.23; N,
14.06; O, 21.97
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Information about this agent
AEZS-108 (previously AN-152) consists of [D-Lys(6)]
LHRH linked to doxorubicin. It is an experimental targeted therapy for
various cancers (ovarian, endometrial, breast, bladder, prostate) that
express LHRH receptor.
AEZS-108 is currently being developed by AEterna-Zentaris. The US FDA
has granted it orphan drug status for ovarian cancer. Promising results
have been reported from a phase II clinical trial for ovarian cancer. It
is also in a phase II trial for endometrial cancer. A Phase I trial for
bladder cancer using AEZS-108 is currently underway at the University of
MIami using a synthetic form of LHRH developed by Dr. Andrew Schally, a
Nobel Prize Laureate. Early results from this trial have shown promise.
Acordingto AEterna-Zentaris's website, After
having successfully completed the Phase 2 trials in ovarian and
endometrial cancer, we expect to initiate a first pivotal trial in
endometrial cancer during 2011. AEZS-108 has been granted orphan-drug
designation by the FDA for ovarian cancer. Furthermore, AEZS-108 is
being investigated in Phase 1/2 trials in prostate and bladder cancer. (source:
1: Gründker C, Ernst J, Reutter MD, Ghadimi BM, Emons
G. Effective targeted chemotherapy using AEZS-108 (AN-152) for LHRH
receptor-positive pancreatic cancers. Oncol Rep. 2011 Sep;26(3):629-35.
doi: 10.3892/or.2011.1340. Epub 2011 Jun 7. PubMed PMID: 21667032.
2: Emons G, Kaufmann M, Gorchev G, Tsekova V, Gründker C, Günthert AR,
Hanker LC, Velikova M, Sindermann H, Engel J, Schally AV. Dose
escalation and pharmacokinetic study of AEZS-108 (AN-152), an LHRH
agonist linked to doxorubicin, in women with LHRH receptor-positive
tumors. Gynecol Oncol. 2010 Dec;119(3):457-61. Epub 2010 Sep 9. PubMed
3: Emons G, Sindermann H, Engel J, Schally AV, Gründker C. Luteinizing
hormone-releasing hormone receptor-targeted chemotherapy using AN-152.
Neuroendocrinology. 2009;90(1):15-8. Epub 2009 Jun 12. PubMed PMID:
4: Engel JB, Keller G, Schally AV, Nagy A, Chism DD, Halmos G. Effective
treatment of experimental human endometrial cancers with targeted
cytotoxic luteinizing hormone-releasing hormone analogues AN-152 and
AN-207. Fertil Steril. 2005 Apr;83 Suppl 1:1125-33. PubMed PMID:
5: Günthert AR, Gründker C, Bongertz T, Nagy A, Schally AV, Emons G.
Induction of apoptosis by AN-152, a cytotoxic analog of luteinizing
hormone-releasing hormone (LHRH), in LHRH-R positive human breast cancer
cells is independent of multidrug resistance-1 (MDR-1) system. Breast
Cancer Res Treat. 2004 Oct;87(3):255-64. PubMed PMID: 15528968.
6: Günthert AR, Gründker C, Bongertz T, Schlott T, Nagy A, Schally AV,
Emons G. Internalization of cytotoxic analog AN-152 of luteinizing
hormone-releasing hormone induces apoptosis in human endometrial and
ovarian cancer cell lines independent of multidrug resistance-1 (MDR-1)
system. Am J Obstet Gynecol. 2004 Oct;191(4):1164-72. PubMed PMID:
7: Letsch M, Schally AV, Szepeshazi K, Halmos G, Nagy A. Preclinical
evaluation of targeted cytotoxic luteinizing hormone-releasing hormone
analogue AN-152 in androgen-sensitive and insensitive prostate cancers.
Clin Cancer Res. 2003 Oct 1;9(12):4505-13. PubMed PMID: 14555524.
8: Bajo AM, Schally AV, Halmos G, Nagy A. Targeted
doxorubicin-containing luteinizing hormone-releasing hormone analogue
AN-152 inhibits the growth of doxorubicin-resistant MX-1 human breast
cancers. Clin Cancer Res. 2003 Sep 1;9(10 Pt 1):3742-8. PubMed PMID:
9: Krebs LJ, Wang X, Nagy A, Schally AV, Prasad PN, Liebow C. Bombesin
and epidermal growth factor potentiate the effect of cytotoxic LH-RH
analog AN-152 in vitro. Int J Oncol. 2002 Dec;21(6):1325-9. PubMed PMID:
10: Gründker C, Völker P, Griesinger F, Ramaswamy A, Nagy A, Schally AV,
Emons G. Antitumor effects of the cytotoxic luteinizing
hormone-releasing hormone analog AN-152 on human endometrial and ovarian
cancers xenografted into nude mice. Am J Obstet Gynecol. 2002
Sep;187(3):528-37. PubMed PMID: 12237622.
11: Westphalen S, Kotulla G, Kaiser F, Krauss W, Werning G, Elsasser HP,
Nagy A, Schulz KD, Grundker C, Schally AV, Emons G. Receptor mediated
antiproliferative effects of the cytotoxic LHRH agonist AN-152 in human
ovarian and endometrial cancer cell lines. Int J Oncol. 2000
Nov;17(5):1063-9. PubMed PMID: 11029513.
12: Nagy A, Plonowski A, Schally AV. Stability of cytotoxic luteinizing
hormone-releasing hormone conjugate (AN-152) containing doxorubicin
14-O-hemiglutarate in mouse and human serum in vitro: implications for
the design of preclinical studies. Proc Natl Acad Sci U S A. 2000 Jan
18;97(2):829-34. PubMed PMID: 10639165; PubMed Central PMCID: PMC15416.
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