Compounds > idn 5390

Page last updated: 2024-11-12

idn 5390

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

IDN 5390: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	9897149
CHEMBL ID	194556
SCHEMBL ID	14023372
MeSH ID	M0431210

Synonyms (4)

Synonym
idn 5390
CHEMBL194556
SCHEMBL14023372
[(1s,2s,4e,9s)-3-[(2r,3s)-3-acetyloxy-2-(2-hydroxyethyl)oxetan-3-yl]-1,5-dihydroxy-9-[(2r,3s)-2-hydroxy-5-methyl-3-[(2-methylpropan-2-yl)oxycarbonylamino]hexanoyl]oxy-4,8,11,11-tetramethyl-6-oxo-2-bicyclo[5.3.1]undeca-4,7-dienyl] benzoate

Research Excerpts

Overview

IDN 5390 is a seco-derivative cytostatic taxane. It has been selected for preclinical development on the basis of its antimotility activity on endothelial cells and antitumour efficacy.

Excerpt	Reference	Relevance
"IDN 5390 is a seco-derivative cytostatic taxane. "	( IDN 5390: a new concept in taxane development. Giavazzi, R; Micheletti, G; Riva, A; Taraboletti, G, 2003)	3.2
"IDN 5390 is a novel C-seco taxane analogue selected for preclinical development on the basis of its antimotility activity on endothelial cells, antitumour efficacy in a large panel of human tumour xenografts and high tolerability in mouse. "	( Antitumour and antiangiogenic effects of IDN 5390, a novel C-seco taxane, in a paclitaxel-resistant human ovarian tumour xenograft. Belluco, S; Cassinelli, G; Favini, E; Lanzi, C; Petrangolini, G; Pratesi, G; Supino, R; Tortoreto, M; Zunino, F, 2004)	2.03

Pharmacokinetics

Excerpt	Reference	Relevance
"In this report, electrospray ionization tandem mass spectrometry (ESI-MS/MS) for a pharmacokinetic study of IDN 5390, a novel C-seco taxane derivative, which is under preclinical evaluation, has been investigated."	( Pharmacokinetic measurements of IDN 5390 using electrospray ionization tandem mass spectrometry: structure characterization and quantification in dog plasma. Bombardelli, E; Kanter, P; Manzotti, C; Morazzoni, P; Pendyala, L; Prey, JD; Song, L; Xue, J, 2005)	0.82
"9 l/kg at, respectively, 60, 90, and 120 mg/kg, and a half-life 24, 36, and 54 min."	( Pharmacokinetics and metabolism in mice of IDN 5390 (13-(N-Boc-3-i-butylisoserinoyl)-C-7,8-seco-10-deacetylbaccatin III), a new oral c-seco-taxane derivative with antiangiogenic property effective on paclitaxel-resistant tumors. Bagnati, R; Colombo, T; D'Incalci, M; Falcioni, C; Fontana, G; Frapolli, R; Manzotti, C; Marangon, E; Morazzoni, P; Simone, M; Zaffaroni, M; Zucchetti, M, 2006)	0.6

Bioavailability

IDN 5390 was rapidly absorbed after oral administration, with good bioavailability (43%). Indeed, a goodBioavailability of oral IDN5390 was found.

Excerpt	Reference	Relevance
" Indeed, a good bioavailability of oral IDN 5390 was found."	( IDN 5390: an oral taxane candidate for protracted treatment schedules. Bombardelli, E; Cassinelli, G; D'Incalci, M; Frapolli, R; Laccabue, D; Lanzi, C; Morazzoni, P; Pratesi, G; Riva, A; Supino, R; Zucchetti, M; Zunino, F, 2003)	2.03
" IDN 5390 was rapidly absorbed after oral administration, with good bioavailability (43%)."	( Pharmacokinetics and metabolism in mice of IDN 5390 (13-(N-Boc-3-i-butylisoserinoyl)-C-7,8-seco-10-deacetylbaccatin III), a new oral c-seco-taxane derivative with antiangiogenic property effective on paclitaxel-resistant tumors. Bagnati, R; Colombo, T; D'Incalci, M; Falcioni, C; Fontana, G; Frapolli, R; Manzotti, C; Marangon, E; Morazzoni, P; Simone, M; Zaffaroni, M; Zucchetti, M, 2006)	1.51

Dosage Studied

Excerpt	Relevance	Reference
" In vivo, IDN 5390 shows activity against paclitaxel-sensitive and -resistant tumors when administered on a prolonged, continuous dosage schedule."	( Pharmacokinetics and metabolism in mice of IDN 5390 (13-(N-Boc-3-i-butylisoserinoyl)-C-7,8-seco-10-deacetylbaccatin III), a new oral c-seco-taxane derivative with antiangiogenic property effective on paclitaxel-resistant tumors. Bagnati, R; Colombo, T; D'Incalci, M; Falcioni, C; Fontana, G; Frapolli, R; Manzotti, C; Marangon, E; Morazzoni, P; Simone, M; Zaffaroni, M; Zucchetti, M, 2006)	1

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Other Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Albumin	Homo sapiens (human)	KD2	1,825.0000	6.0000	6.0000	6.0000	AID239810
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (5)

Process	via Protein(s)	Taxonomy
cellular response to starvation	Albumin	Homo sapiens (human)
negative regulation of mitochondrial depolarization	Albumin	Homo sapiens (human)
cellular response to calcium ion starvation	Albumin	Homo sapiens (human)
cellular oxidant detoxification	Albumin	Homo sapiens (human)
transport	Albumin	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Process	via Protein(s)	Taxonomy
oxygen binding	Albumin	Homo sapiens (human)
DNA binding	Albumin	Homo sapiens (human)
fatty acid binding	Albumin	Homo sapiens (human)
copper ion binding	Albumin	Homo sapiens (human)
protein binding	Albumin	Homo sapiens (human)
toxic substance binding	Albumin	Homo sapiens (human)
antioxidant activity	Albumin	Homo sapiens (human)
pyridoxal phosphate binding	Albumin	Homo sapiens (human)
identical protein binding	Albumin	Homo sapiens (human)
protein-folding chaperone binding	Albumin	Homo sapiens (human)
exogenous protein binding	Albumin	Homo sapiens (human)
enterobactin binding	Albumin	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (11)

Process	via Protein(s)	Taxonomy
extracellular region	Albumin	Homo sapiens (human)
extracellular space	Albumin	Homo sapiens (human)
nucleus	Albumin	Homo sapiens (human)
endoplasmic reticulum	Albumin	Homo sapiens (human)
endoplasmic reticulum lumen	Albumin	Homo sapiens (human)
Golgi apparatus	Albumin	Homo sapiens (human)
platelet alpha granule lumen	Albumin	Homo sapiens (human)
extracellular exosome	Albumin	Homo sapiens (human)
blood microparticle	Albumin	Homo sapiens (human)
protein-containing complex	Albumin	Homo sapiens (human)
cytoplasm	Albumin	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (14)

Assay ID	Title	Year	Journal	Article
AID422268	Cytotoxicity against human A2780/ADR cells after 72 hrs	2009	Journal of natural products, Mar-27, Volume: 72, Issue:3	Recent advances in the chemistry and biology of new generation taxoids.
AID422270	Cytotoxicity against human paclitaxel and cyclosporine-resistant A2780TC3 cells overexpressing class 3 beta-tubulin after 72 hrs	2009	Journal of natural products, Mar-27, Volume: 72, Issue:3	Recent advances in the chemistry and biology of new generation taxoids.
AID239809	Equilibrium dissociation constant for the interaction between the compound and serum albumin	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions.
AID422265	Cytotoxicity against human wild type A2780 cells after 72 hrs	2009	Journal of natural products, Mar-27, Volume: 72, Issue:3	Recent advances in the chemistry and biology of new generation taxoids.
AID422271	Activity ratio of compound IC50 to paclitaxel IC50 for paclitaxel and cyclosporine-resistant human A2780TC3 cells overexpressing class 3 beta-tubulin	2009	Journal of natural products, Mar-27, Volume: 72, Issue:3	Recent advances in the chemistry and biology of new generation taxoids.
AID242932	Dissociation rate constant for the interaction between the compound and serum albumin	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions.
AID242933	Dissociation rate constant for the interaction between the compound and serum albumin	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions.
AID422272	Resistance factor, ratio of IC50 for paclitaxel and cyclosporine-resistant human A2780TC3 cells overexpressing class 3 beta-tubulin to IC50 for wild type human A2780 cells	2009	Journal of natural products, Mar-27, Volume: 72, Issue:3	Recent advances in the chemistry and biology of new generation taxoids.
AID242868	Association rate constant for the interaction between the compound and serum albumin	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions.
AID422269	Cytotoxicity against human paclitaxel and cyclosporine-resistant A2780TC1 cells overexpressing class 3 beta-tubulin after 72 hrs	2009	Journal of natural products, Mar-27, Volume: 72, Issue:3	Recent advances in the chemistry and biology of new generation taxoids.
AID239810	Equilibrium dissociation constant for the interaction between the compound and serum albumin	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions.
AID422266	Cytotoxicity against human cisplatin-resistant A2780 cells after 72 hrs	2009	Journal of natural products, Mar-27, Volume: 72, Issue:3	Recent advances in the chemistry and biology of new generation taxoids.
AID422267	Cytotoxicity against human topotecan-resistant A2780 cells after 72 hrs	2009	Journal of natural products, Mar-27, Volume: 72, Issue:3	Recent advances in the chemistry and biology of new generation taxoids.
AID242869	Association rate constant for the interaction between the compound and serum albumin	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (13)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	12 (92.31)	29.6817
2010's	1 (7.69)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.60

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

Metric	This Compound (vs All)
Research Demand Index	11.60 (24.57)
Research Supply Index	2.64 (2.92)
Research Growth Index	4.24 (4.65)
Search Engine Demand Index	0.00 (26.88)
Search Engine Supply Index	0.00 (0.95)

This Compound (11.60)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	2 (15.38%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	11 (84.62%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
paclitaxel Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).	4.63	8	0	taxane diterpenoid; tetracyclic diterpenoid	antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent
nelfinavir Nelfinavir: A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.. nelfinavir : An aryl sulfide that is used (as its mesylate salt) for treatment of HIV and also exhibits some anticancer properties.	2.02	1	0	aryl sulfide; benzamides; organic heterobicyclic compound; phenols; secondary alcohol; tertiary amino compound	antineoplastic agent; HIV protease inhibitor
amprenavir [no description available]	2.02	1	0	carbamate ester; sulfonamide; tetrahydrofuryl ester	antiviral drug; HIV protease inhibitor
lopinavir [no description available]	2.02	1	0	amphetamines; dicarboxylic acid diamide	anticoronaviral agent; antiviral drug; HIV protease inhibitor
docetaxel [no description available]	3.54	2	0	hydrate; secondary alpha-hydroxy ketone	antineoplastic agent
docetaxel anhydrous Docetaxel: A semisynthetic analog of PACLITAXEL used in the treatment of locally advanced or metastatic BREAST NEOPLASMS and NON-SMALL CELL LUNG CANCER.. docetaxel anhydrous : A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group.	2.21	1	0	secondary alpha-hydroxy ketone; tetracyclic diterpenoid	antimalarial; antineoplastic agent; photosensitizing agent
atazanavir atazanavir : A heavily substituted carbohydrazide that is an antiretroviral drug of the protease inhibitor (PI) class used to treat infection of human immunodeficiency virus (HIV).	2.02	1	0	carbohydrazide	antiviral drug; HIV protease inhibitor
ritonavir Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.	2.02	1	0	1,3-thiazoles; carbamate ester; carboxamide; L-valine derivative; ureas	antiviral drug; environmental contaminant; HIV protease inhibitor; xenobiotic
saquinavir Saquinavir: An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.. saquinavir : An aspartic acid derivative obtained by formal condensation of the primary amino group of (2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl]-3-hydroxy-1-phenylbutan-2-ylamine with the carboxy group of N(2)(-quinolin-2-ylcarbonyl)-L-asparagine. An inhibitor of HIV-1 protease.	2.02	1	0	L-asparagine derivative; quinolines	antiviral drug; HIV protease inhibitor
indinavir sulfate Indinavir: A potent and specific HIV protease inhibitor that appears to have good oral bioavailability.	2.02	1	0	dicarboxylic acid diamide; N-(2-hydroxyethyl)piperazine; piperazinecarboxamide	HIV protease inhibitor
idn 5109 IDN 5109: structure in first source	2.02	1	0
taxane taxane: produced by Taxomyces andreanae	7.01	1	0	diterpene; terpenoid fundamental parent
sb t-1213 [no description available]	3.14	1	0
sb t-1214 [no description available]	3.14	1	0

Condition	Indicated	Relationship Strength	Studies	Trials
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	0	2.01	1	0
Benign Neoplasms, Brain [description not available]	0	2.01	1	0
Carcinoma, Anaplastic [description not available]	0	2.01	1	0
Cancer of Colon [description not available]	0	2.01	1	0
Astrocytoma, Grade IV [description not available]	0	2.01	1	0
Experimental Neoplasms [description not available]	0	2.01	1	0
Cancer of Ovary [description not available]	0	2.71	3	0
Brain Neoplasms Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.	0	2.01	1	0
Carcinoma A malignant neoplasm made up of epithelial cells tending to infiltrate the surrounding tissues and give rise to metastases. It is a histological type of neoplasm and not a synonym for cancer.	0	2.01	1	0
Colonic Neoplasms Tumors or cancer of the COLON.	0	2.01	1	0
Glioblastoma A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.	0	2.01	1	0
Ovarian Neoplasms Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.	0	2.71	3	0
Metastase [description not available]	0	2.93	1	0
Benign Neoplasms [description not available]	0	2.93	1	0
Neoplasm Metastasis The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.	0	2.93	1	0
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	0	2.93	1	0
Cancer of Lung [description not available]	0	2.01	1	0
B16 Melanoma [description not available]	0	2.01	1	0
Lung Neoplasms Tumors or cancer of the LUNG.	0	2.01	1	0