ZOPTARELIN DOXORUBICIN

First approved in 1974

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C91H117N19O26
Molecular Weight	1893.0144
Optical Activity	UNSPECIFIED
Defined Stereocenters	15 / 15
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[H][C@@]1(C[C@H](N)[C@H](O)[C@H](C)O1)O[C@H]2C[C@@](O)(CC3=C(O)C4=C(C(=O)C5=C(OC)C=CC=C5C4=O)C(O)=C23)C(=O)COC(=O)CCCC(=O)NCCCC[C@@H](NC(=O)[C@H](CC6=CC=C(O)C=C6)NC(=O)[C@H](CO)NC(=O)[C@H](CC7=CNC8=C7C=CC=C8)NC(=O)[C@H](CC9=CN=CN9)NC(=O)[C@@H]%10CCC(=O)N%10)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N%11CCC[C@H]%11C(=O)NCC(N)=O

InChI

InChIKey=OOUACICUAVTCEC-LZHWUUGESA-N

InChI=1S/C91H117N19O26/c1-44(2)31-58(83(125)104-57(17-11-29-98-90(94)95)89(131)110-30-12-18-63(110)88(130)100-40-67(93)114)105-81(123)55(16-7-8-28-97-68(115)20-10-21-70(117)134-42-66(113)91(132)36-52-73(65(37-91)136-71-35-53(92)76(118)45(3)135-71)80(122)75-74(78(52)120)77(119)51-14-9-19-64(133-4)72(51)79(75)121)103-84(126)59(32-46-22-24-49(112)25-23-46)106-87(129)62(41-111)109-85(127)60(33-47-38-99-54-15-6-5-13-50(47)54)107-86(128)61(34-48-39-96-43-101-48)108-82(124)56-26-27-69(116)102-56/h5-6,9,13-15,19,22-25,38-39,43-45,53,55-63,65,71,76,99,111-112,118,120,122,132H,7-8,10-12,16-18,20-21,26-37,40-42,92H2,1-4H3,(H2,93,114)(H,96,101)(H,97,115)(H,100,130)(H,102,116)(H,103,126)(H,104,125)(H,105,123)(H,106,129)(H,107,128)(H,108,124)(H,109,127)(H4,94,95,98)/t45-,53-,55+,56-,57-,58-,59-,60-,61-,62-,63-,65-,71-,76+,91-/m0/s1

HIDE SMILES / InChI

Description
Sources: http://www.drugbank.ca/drugs/DB00997http://www.cytrx.com/aldoxorubicin
Curator's Comment: The description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/28846045 | https://clinicaltrials.gov/ct2/show/NCT02049905 | https://www.ncbi.nlm.nih.gov/pubmed/26378637 | https://clinicaltrials.gov/ct2/show/NCT02014844 | https://www.ncbi.nlm.nih.gov/pubmed/25312684 | https://clinicaltrials.gov/ct2/show/NCT02200757

Aldoxorubicin (INNO-206) is a tumor-targeted doxorubicin conjugate developed by CytRx for treating relapsed and refractory sarcomas, especially L-sarcomas. Aldoxorubicin is a rationally-engineered cytotoxic which delivers a well-established anti-cancer agent, doxorubicin, into the tumor. Currently, in late-stage clinical trials, Aldoxorubicin appears to overcome the key limitations of doxorubicin, including cumulative dose restrictions. Aldoxorubicin utilizes an acid-sensitive linker that selectively binds to albumin, which may allow the cytotoxic payload to preferentially accumulate in the tumor and potentially spare the surrounding healthy tissue. This mechanism leverages the tumor's low pH environment and accompanying dependency upon circulating albumin to fuel growth, to enable the delivery of multifold times the standard dosing of doxorubicin. The preferential uptake of Aldoxorubicin by tumor tissue and the acid sensitive release of doxorubicin allow for Aldoxorubicin to be a very promising anticancer agent. In phase I and II trials, Aldoxorubicin demonstrates superior efficacy over doxorubicin. Although the studies were not powered for OS, Aldoxorubicin shows improved PFS and tumor response in comparison to doxorubicin. The safety profile was also comparable to that of doxorubicin. Similarly, results from the recent phase III study showed a benefit in PFS in the leiomyosarcoma subtypes.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
DNA topoisomerase II 66 Target ID: CHEMBL2094255 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28846045	Inhibitor 8297	2.67 µM [IC50]
Serum albumin 18 Target ID: CHEMBL3253 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28846045	Binding Agent 1064
DNA topoisomerase II alpha 37 Target ID: CHEMBL1806 Sources: http://www.drugbank.ca/drugs/DB00997	Inhibitor 8297
DNA topoisomerase II 66 Target ID: CHEMBL2094255 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17194596	Inhibitor 8297	2.67 µM [IC50]
A673 8 Target ID: CHEMBL614517 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27688190	Inhibitor 8297	200.0 nM [IC50]
HepG2 16 Target ID: CHEMBL395 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27669220	Inhibitor 8297	24.68 µM [IC50]
Human ovarian cancer cell line 8 Target ID: CHEMBL613895 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26694484	Inhibitor 8297	0.074 µM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Locally advanced or unresectable soft tissue sarcoma 8 Sources: https://clinicaltrials.gov/ct2/show/NCT02049905	Primary	Phase III 656	Unknown Approved Use Unknown
Kaposi’s sarcoma 13 Sources: https://clinicaltrials.gov/ct2/show/NCT02029430	Primary	Phase II 1132	Unknown Approved Use Unknown
Glioblastoma 65 Sources: https://clinicaltrials.gov/ct2/show/NCT02014844	Primary	Phase II 1132	Unknown Approved Use Unknown
Metastatic non-small cell lung cancer 13 Sources: https://clinicaltrials.gov/ct2/show/NCT02200757	Primary	Phase II 1132	Unknown Approved Use Unknown
Pancreatic ductal adenocarcinoma 14 Sources: https://clinicaltrials.gov/ct2/show/NCT01580397	Primary	Phase II 1132	Unknown Approved Use Unknown
Ovarian cancer 157 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/050718s045lbl.pdf	Primary	Approved 8429	DOXIL Approved Use Indicated for: Ovarian cancer After failure of platinum-based chemotherapy. AIDS-related Kaposi’s Sarcoma After failure of prior systemic chemotherapy or intolerance to such therapy. Multiple Myeloma Launch Date 1995
AIDS-related Kaposi’s sarcoma 15 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/050718s045lbl.pdf	Primary	Approved 8429	DOXIL Approved Use Indicated for: Ovarian cancer After failure of platinum-based chemotherapy. AIDS-related Kaposi’s Sarcoma After failure of prior systemic chemotherapy or intolerance to such therapy. Multiple Myeloma Launch Date 1995
Multiple myeloma 159 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/050718s045lbl.pdf	Primary	Approved 8429	DOXIL Approved Use Indicated for: Ovarian cancer After failure of platinum-based chemotherapy. AIDS-related Kaposi’s Sarcoma After failure of prior systemic chemotherapy or intolerance to such therapy. Multiple Myeloma Launch Date 1995

C_max

Value	Dose	Co-administered	Analyte	Population
2 μM EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/26115930	60 mg/m² 1 times / day steady-state, intravenous dose: 60 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered:		DOXORUBICIN plasma	Homo sapiens population: UNHEALTHY age: CHILD sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
7.4 μM × h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/26115930	60 mg/m² 1 times / day steady-state, intravenous dose: 60 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered:		DOXORUBICIN plasma	Homo sapiens population: UNHEALTHY age: CHILD sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
34.8 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/26115930	60 mg/m² 1 times / day steady-state, intravenous dose: 60 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered:		DOXORUBICIN plasma	Homo sapiens population: UNHEALTHY age: CHILD sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
25% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/050467s073lbl.pdf			DOXORUBICIN plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
150 mg/m2 1 times / day multiple, intravenous Overdose Dose: 150 mg/m2, 1 times / day Route: intravenous Route: multiple Dose: 150 mg/m2, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/050467s078,050629s030lbl.pdf	unhealthy, 17 years n = 1 Health Status: unhealthy Age Group: 17 years Sex: F Population Size: 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/050467s078,050629s030lbl.pdf	Other AEs: Mucositis, Chills... Other AEs: Mucositis (severe, 1 patient) Chills (1 patient) Pyrexia (1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/050467s078,050629s030lbl.pdf
300 mg/m2 single, intravenous Overdose Dose: 300 mg/m2 Route: intravenous Route: single Dose: 300 mg/m2 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/050467s078,050629s030lbl.pdf	unhealthy, 58 years n = 1 Health Status: unhealthy Condition: acute lymphoblastic leukemia Age Group: 58 years Sex: M Population Size: 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/050467s078,050629s030lbl.pdf	Other AEs: Sinus tachycardia, Neutropenia... Other AEs: Sinus tachycardia (1 patient) Neutropenia (grade 4, 1 patient) Thrombocytopenia (1 patient) Mucositis (severe, 1 patient) Sepsis (severe, 1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/050467s078,050629s030lbl.pdf
60 mg/m2 1 times / 3 weeks multiple, intravenous Recommended Dose: 60 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 60 mg/m2, 1 times / 3 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/050467s078,050629s030lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/050467s078,050629s030lbl.pdf	Disc. AE: Tissue injury... Other AEs: Acute myeloid leukaemia, Myelodysplastic syndrome... AEs leading to discontinuation/dose reduction: Tissue injury (severe) Other AEs: Acute myeloid leukaemia Myelodysplastic syndrome Myelosuppression (severe) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/050467s078,050629s030lbl.pdf
300 mg/m2 1 times / 3 weeks multiple, intravenous (total) Dose: 300 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 300 mg/m2, 1 times / 3 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/050467s078,050629s030lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/050467s078,050629s030lbl.pdf	Other AEs: Cardiomyopathy... Other AEs: Cardiomyopathy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/050467s078,050629s030lbl.pdf
450 mg/m2 1 times / 3 weeks multiple, intravenous Highest studied dose Dose: 450 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 450 mg/m2, 1 times / 3 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25312684 Page: p.574	unhealthy, ADULT n = 2 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: F Food Status: UNKNOWN Population Size: 2 Sources: https://pubmed.ncbi.nlm.nih.gov/25312684 Page: p.574	DLT: Neutropenia, Febrile neutropenia... Disc. AE: Anemia, Neutropenia... Dose limiting toxicities: Neutropenia (grade 4, 50%) Febrile neutropenia (grade 3, 50%) AEs leading to discontinuation/dose reduction: Anemia (grade 3, 50%) Neutropenia (grade 3, 50%) Sources: https://pubmed.ncbi.nlm.nih.gov/25312684 Page: p.574
350 mg/m2 1 times / 3 weeks multiple, intravenous MTD Dose: 350 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 350 mg/m2, 1 times / 3 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25312684 Page: p.574	unhealthy, ADULT n = 18 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 18 Sources: https://pubmed.ncbi.nlm.nih.gov/25312684 Page: p.574	DLT: Dehydration, Neutropenia... Disc. AE: Septic shock, Anemia... Dose limiting toxicities: Dehydration (5.6%) Neutropenia (5.6%) Sepsis (5.6%) AEs leading to discontinuation/dose reduction: Septic shock (grade 5, 5.6%) Anemia (grade 3, 5.6%) Sources: https://pubmed.ncbi.nlm.nih.gov/25312684 Page: p.574

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
	P-gp 1537 AKR1C3 13 NDUFS2 8 NDUFS3 8 NDUFS7 8 NQO1 8 XDH 8 MRP1 107 MRP2 205 BCRP 561 SLC22A16 8 MRP5 40 OATP1A2 62 OATP1B1 406 OATP1B3 350	CYP1A1 108 CYP1A2 701 CYP1B1 51 CYP2B2 15 CYP2E1 128 CYP2J3 8 CYP2C11 14 CYP2B1 26 CYP2C23 10

Drug as perpetrator

Target	Modality	Activity
CYP2B1 41	inducer 1573 Sources: https://www.sciencedirect.com/science/article/pii/S1537189108000864 Page: -	no
CYP2C23 10	inducer 1573 Sources: https://www.sciencedirect.com/science/article/pii/S1537189108000864 Page: -	no
CYP2C11 15	inducer 1573 Sources: https://www.sciencedirect.com/science/article/pii/S1537189108000864 Page: -	weak
CYP1A1 218	inducer 1573 Sources: https://www.sciencedirect.com/science/article/pii/S1537189108000864 Page: -	yes
CYP1A2 1692	inducer 1573 Sources: https://www.sciencedirect.com/science/article/pii/S1537189108000864 Page: -	yes
CYP1B1 67	inducer 1573 Sources: https://www.sciencedirect.com/science/article/pii/S1537189108000864 Page: -	yes
CYP2B2 16	inducer 1573 Sources: https://www.sciencedirect.com/science/article/pii/S1537189108000864 Page: -	yes
CYP2E1 970	inducer 1573 Sources: https://www.sciencedirect.com/science/article/pii/S1537189108000864 Page: -	yes
CYP2J3 8	inducer 1573 Sources: https://www.sciencedirect.com/science/article/pii/S1537189108000864 Page: -	yes

Drug as victim

Target	Modality	Activity	Metabolite
SLC22A16 8	substrate 3367 Sources: https://www.sciencedirect.com/science/article/pii/S0006291X05011873 Page: -	yes [Km 5.2 uM]
AKR1C3 13	substrate 3367 Sources: https://www.pharmgkb.org/literature/8369411 Page: -	yes
BCRP 561	substrate 3367 Sources: https://www.pharmgkb.org/pathway/PA165292177 Page: -	yes
MRP1 107	substrate 3367 Sources: https://www.pharmgkb.org/pathway/PA165292177 Page: -	yes
MRP2 205	substrate 3367 Sources: https://www.pharmgkb.org/pathway/PA165292177 Page: -	yes
MRP5 40	substrate 3367 Sources: https://www.sciencedirect.com/science/article/pii/S0378427401003915 Page: -	yes	GS-DOX 8
NDUFS2 8	substrate 3367 Sources: https://www.pharmgkb.org/pathway/PA165292177 Page: -	yes
NDUFS3 8	substrate 3367 Sources: https://www.pharmgkb.org/pathway/PA165292177 Page: -	yes
NDUFS7 8	substrate 3367 Sources: https://www.pharmgkb.org/pathway/PA165292177 Page: -	yes
NQO1 8	substrate 3367 Sources: https://www.pharmgkb.org/pathway/PA165292177 Page: -	yes
OATP1A2 62	substrate 3367 Sources: https://www.sciencedirect.com/science/article/pii/S0378427401003915 Page: -	yes
OATP1B1 406	substrate 3367 Sources: https://www.sciencedirect.com/science/article/pii/S0378427401003915 Page: -	yes
OATP1B3 350	substrate 3367 Sources: https://www.sciencedirect.com/science/article/pii/S0378427401003915 Page: -	yes
P-gp 1537	substrate 3367 Sources: https://link.springer.com/article/10.1007/s12272-011-0411-x Page: -	yes
XDH 8	substrate 3367 Sources: https://www.pharmgkb.org/pathway/PA165292177 Page: -	yes

Sourcing

Vendor/Aggregator	ID	URL
AbovChem LLC	HY-16261A	http://www.abovchem.com/pc/en/product_list.aspx?wd=HY-16261A
BLD Pharm	BD630336	http://www.bldpharm.com/search/Search.html?keyword=BD630336
ChEBI	CHEBI:28748	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:28748
Chem Scene	CS-0077171	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-0077171
MedChem Express	HY-16261B	https://www.medchemexpress.com/search.html?q=HY-16261B&ft=&fa=&fp=
MolPort	MolPort-006-124-025	https://www.molport.com/shop/molecule-link/MolPort-006-124-025
ZINC	ZINC000003918087	http://zinc15.docking.org/substances/ZINC000003918087
eMolecules	50284280	https://orderbb.emolecules.com/search/#?query=50284280
eMolecules	36788175	https://www.emolecules.com/cgi-bin/more?vid=36788175
mcule	MCULE-8506890923	https://mcule.com/MCULE-8506890923/

PubMed

Title	Date	PubMed
Protective effects of carvedilol against doxorubicin-induced cardiomyopathy in rats.	1999	10503942
Topical DMSO treatment for pegylated liposomal doxorubicin-induced palmar-plantar erythrodysesthesia.	1999	10447577
Use of dexrazoxane as a cardioprotectant in patients receiving doxorubicin or epirubicin chemotherapy for the treatment of cancer. The Provincial Systemic Treatment Disease Site Group.	1999 Apr	10474762
Anticancer drug sensitivity and expression of multidrug resistance markers in early passage human sarcomas.	1999 Aug	10473106
Doxorubicin-induced cardiomyopathy.	1999 Feb 25	10049085
[Changes in left ventricular function during chemotherapy with doxorubicin].	1999 Jul	11045157
Doxorubicin cardiotoxicity: growing importance.	1999 Jul	10561289
Effect of proteinuria reduction on prevention of focal glomerulosclerosis by angiotensin-converting enzyme inhibition is modifiable.	1999 Jul	10412735
Effect of captopril on doxorubicin-induced nephrotoxicity in normal rats.	1999 Mar	10094850
Delayed methotrexate clearance in a patient with sickle cell anemia and osteosarcoma.	1999 Mar-Apr	10206466
Dose-finding study of docetaxel and doxorubicin in first-line treatment of patients with metastatic breast cancer.	1999 May	10416005
Phase II trial of high-dose liposome-encapsulated doxorubicin with granulocyte colony-stimulating factor in metastatic breast cancer. TLC D-99 Study Group.	1999 May	10334528
Low-dose vincristine-associated bilateral vocal cord paralysis.	1999 Oct	10578547
Renal protective effects of blocking the intrarenal renin-angiotensin system.	1999 Sep	10515446
Doxorubicin-induced late cardiotoxicity: delayed impairment of Ca2+-handling mechanisms in the sarcoplasmic reticulum in the rat.	2000 Apr	10772060
Glomerular basement membrane anionic sites in adriamycin nephropathy: effect of saline loading and nitric oxide modulation.	2000 Apr	10754413
Anthracyclines trigger apoptosis of both G0-G1 and cycling peripheral blood lymphocytes and induce massive deletion of mature T and B cells.	2000 Apr 1	10766178
Pegylated liposomal doxorubicin (doxil): reduced clinical cardiotoxicity in patients reaching or exceeding cumulative doses of 500 mg/m2.	2000 Aug	11038041
The protective effect of glutathione administration on adriamycin-induced acute cardiac toxicity in rats.	2000 Aug	10887039
Progressive cardiac dysfunction in adriamycin-induced cardiomyopathy rats.	2000 Dec	11113713
High incidence of adriamycin cardiotoxicity in children even at low cumulative doses: role of radionuclide cardiac angiography.	2000 Dec	11101737
Proteasome-mediated degradation of the coactivator p300 impairs cardiac transcription.	2000 Dec	11073966
Neural crest-derived defects in experimental esophageal atresia.	2000 Feb	10674343
Curcumin prevents adriamycin nephrotoxicity in rats.	2000 Jan	10694226
Comparison of doxorubicin- and MEN 10755-induced long-term progressive cardiotoxicity in the rat.	2000 Jan	10630739
Liposomal doxorubicin (Caelyx) in advanced pretreated soft tissue sarcomas: a phase II study of the Italian Sarcoma Group (ISG).	2000 Jan-Feb	10769710
Doxorubicin-induced cardiomyopathy.	2000 Jul	10910374
Cardiac peroxynitrite formation and left ventricular dysfunction following doxorubicin treatment in mice.	2000 Jul	10871338
Effects of probucol on changes of antioxidant enzymes in adriamycin-induced cardiomyopathy in rats.	2000 Jun	10912462
Evaluation of cardiac adrenergic neuronal damage in rats with doxorubicin-induced cardiomyopathy using iodine-131 MIBG autoradiography and PGP 9.5 immunohistochemistry.	2000 Jun	10901455
Deficiency of the stress kinase p38alpha results in embryonic lethality: characterization of the kinase dependence of stress responses of enzyme-deficient embryonic stem cells.	2000 Mar 6	10704466
The influence of thymoquinone on doxorubicin-induced hyperlipidemic nephropathy in rats.	2000 Mar 7	10755708
Expression of agrin, dystroglycan, and utrophin in normal renal tissue and in experimental glomerulopathies.	2000 May	10793086
Bilateral blindness and lumbosacral myelopathy associated with high-dose carmustine and cisplatin therapy.	2000 Sep	11020424
Long-term cardiac sequelae in operable breast cancer patients given adjuvant chemotherapy with or without doxorubicin and breast irradiation.	2001 Jan 1	11134193
Human mismatch repair and G*T mismatch binding by hMutSalpha in vitro is inhibited by adriamycin, actinomycin D, and nogalamycin.	2001 Mar 30	11134041

Patents

Sample Use Guides

In Vivo Use Guide

When used in combination with other chemotherapy drugs, the most commonly used dosage of doxorubicin is 40 to 60 mg/m2 IV every 21 to 28 days. Alternatively, 60 to 75 mg/m2 IV once every 21 days.

Route of Administration: Intravenous

In Vitro Use Guide

Alkalinization of extracellular pH by urease (2 U/ml) and urea (> or = 2 mM) was found to enhance the antitumor efficacy of doxorubicin (50 uM)

Name

Type

Language

ZOPTARELIN DOXORUBICIN

Official Name

English

LUTEINIZING HORMONE-RELEASING FACTOR (SWINE), 6-(N6-(5-(2-((2S,4S)-4-((3-AMINO-2,3,6-TRIDEOXY-.ALPHA.-L-LYXO-HEXOPYRANOSYL)OXY)-1,2,3,4,6,11-HEXAHYDRO-2,5,12-TRIHYDROXY-7-METHOXY-6,11-DIOXO-2-NAPHTHACENYL)-2-OXOETHOXY)-1,5-DIOXOPENTYL)-D-LYSINE)-

Systematic Name

English

Zoptarelin doxorubicin [WHO-DD]

Common Name

English

LUTEINIZING HORMONE-RELEASING FACTOR (PIG), 6-(N6-(5-(2-(4-((3-AMINO-2,3,6-TRIDEOXY-.ALPHA.-L-LYXO-HEXOPYRANOSYL)OXY)-1,2,3,4,6,11-HEXAHYDRO-2,5,12-TRIHYDROXY-7-METHOXY-6,11-DIOXO-2-NAPHTHACENYL)-2-OXOETHOXY)-1,5-DIOXOPENTYL)-D-LYSINE)-, (2S-CIS)-

Systematic Name

English

(6-D-LYSINE)HUMAN GONADOLIBERIN-1 (LHRH) AND DOXORUBICIN COVALENTLY LINKED TOGETHER WITH GLUTARIC ACID: 5-OXO-L-PROLYL-L-HISTIDYL-L-TRYPTOPHYL-L-SERYL-L-TYROSYL-N6-(5-(2-((2S,4S)-4-((3-AMINO-2,3,6-TRIDEOXY-.ALPHA.-L-LYXO-HEXOPYRANOSYL)OXY)-2,5,12-TRIHYDR

Systematic Name

English

zoptarelin doxorubicin [INN]

Common Name

English

ZOPTARELIN DOXORUBICIN [USAN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C67502