krn 5500 profile

KRN 5500: a derivative of spicamycin with a wide range of antitumor activity against human cancer cell lines; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	6440176
CHEMBL ID	4296683
SCHEMBL ID	2357505
MeSH ID	M0243648

Synonym
krn 5500
l-glycero-beta-l-manno-heptopyranosylamine, 4-deoxy-4-((((1-oxo-2,4-tetradecadienyl)amino)acetyl)amino)-n-1h-purin-6-yl-, (e,e)-
8vh13l5k20 ,
nsc 650426
unii-8vh13l5k20
6-(4-deoxy-4-((2e,4e)-tetradecadienoylglycyl)amino-l-glycero-b-l-mannoheptopyranosyl)amino-9h-purine
l-glycero-beta-l-manno-heptopyranosylamine, 4-deoxy-4-(((((2e,4e)-1-oxo-2,4-tetradecadienyl)amino)acetyl)amino)-n-1h-purin-6-yl-
SCHEMBL2357505
DTXSID60873333
DB15215
CHEMBL4296683
HY-13659
CS-0007543
AKOS040748681

Excerpt	Reference	Relevance
" This study has been conducted to examine whether incorporation of KRN5500 into polymeric micelles (KRN/m) could reduce the toxic effects caused by the current formulation of KRN5500."	( Incorporation of the anticancer agent KRN5500 into polymeric micelles diminishes the pulmonary toxicity. Kakizoe, T; Kawaguchi, T; Matsumura, Y; Mizumura, Y; Moriyasu, F; Okano, T; Yokoyama, M, 2002)	0.31

Excerpt	Reference	Relevance
" The objective of this study was to develop a population pharmacokinetic model that describes the KRN5500 plasma concentration versus time data."	( Population pharmacokinetic modeling and model validation of a spicamycin derivative, KRN5500, in phase 1 study. Sudo, T; Takama, H; Tamura, T; Tanaka, H; Tanigawara, Y, 2001)	0.31
" In addition, the basic and final population pharmacokinetic models were evaluated using bootstrapping resampling."	( Population pharmacokinetic modeling and model validation of a spicamycin derivative, KRN5500, in phase 1 study. Sudo, T; Takama, H; Tamura, T; Tanaka, H; Tanigawara, Y, 2001)	0.31
"The KRN5500 plasma concentration versus time data obtained from the phase 1 study were well described by the population pharmacokinetic model."	( Population pharmacokinetic modeling and model validation of a spicamycin derivative, KRN5500, in phase 1 study. Sudo, T; Takama, H; Tamura, T; Tanaka, H; Tanigawara, Y, 2001)	0.31
" Pharmacokinetic evaluation was performed at the first cycle."	( Phase I and pharmacokinetic study of KRN5500, a spicamycin derivative, for patients with advanced solid tumors. Kamiya, Y; Kondoh, H; Matsumura, Y; Ono, H; Shimada, Y; Shirao, K; Tamura, T; Tanigawara, Y; Yamamoto, N, 2003)	0.32

Assay ID	Title	Year	Journal	Article
AID680079	TP_TRANSPORTER: inhibition of Azidopine photoaffinity labelling (Azidopine: 0.4 uM, KRN5500: 400 uM) in membrane fraction from MDR1-expressing LLC-PK1 cell	2000	Japanese journal of cancer research : Gann, Feb, Volume: 91, Issue:2	The novel anticancer drug KRN5500 interacts with, but is hardly transported by, human P-glycoprotein.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	10 (38.46)	18.2507
2000's	14 (53.85)	29.6817
2010's	2 (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]

Publication Type	This drug (%)	All Drugs (%)
Trials	5 (19.23%)	5.53%
Reviews	3 (11.54%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	18 (69.23%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
A Phase 2 Double-Blind Dose Escalation Study of KRN5500 for Neuropathic Pain in Patients With Cancer [NCT00474916]	Phase 2	19 participants (Actual)	Interventional	2006-06-30	Completed
Phase I Evaluation of KRN5500 (NSC650426) [NCT00002923]	Phase 1	27 participants (Anticipated)	Interventional	1997-05-31	Completed
A Phase I Trial of KRN5500 (NSC 650426) Given as a 72 Hour Continuous IV Infusion Every 21 Days in Patients With Solid Tumors [NCT00017238]	Phase 1	40 participants (Actual)	Interventional	2002-02-28	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Substance	Relationship Strength	Studies	Classes	Roles
mitomycin Mitomycin: An antineoplastic antibiotic produced by Streptomyces caespitosus. It is one of the bi- or tri-functional ALKYLATING AGENTS causing cross-linking of DNA and inhibition of DNA synthesis.. mitomycin : A family of aziridine-containing natural products isolated from Streptomyces caespitosus or Streptomyces lavendulae.	3.49	2	mitomycin	alkylating agent; antineoplastic agent
mannose mannopyranose : The pyranose form of mannose.	1.99	1	D-aldohexose; D-mannose; mannopyranose	metabolite
camptothecin NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source	3.09	1	delta-lactone; pyranoindolizinoquinoline; quinoline alkaloid; tertiary alcohol	antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor; genotoxin; plant metabolite
azides Azides: Organic or inorganic compounds that contain the -N3 group.. azide : Any nitrogen molecular entity containing the group -N3.	2	1	pseudohalide anion	mitochondrial respiratory-chain inhibitor
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).	3.09	1	taxane diterpenoid; tetracyclic diterpenoid	antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent
etoposide [no description available]	2	1	beta-D-glucoside; furonaphthodioxole; organic heterotetracyclic compound	antineoplastic agent; DNA synthesis inhibitor
irinotecan [no description available]	3.09	1	carbamate ester; delta-lactone; N-acylpiperidine; pyranoindolizinoquinoline; ring assembly; tertiary alcohol; tertiary amino compound	antineoplastic agent; apoptosis inducer; EC 5.99.1.2 (DNA topoisomerase) inhibitor; prodrug
glucose, (beta-d)-isomer beta-D-glucose : D-Glucopyranose with beta configuration at the anomeric centre.. (1->4)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->4) linkages.. (1->3)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->3) linkages.	3.09	1	D-glucopyranose	epitope; mouse metabolite
7-hydroxystaurosporine [no description available]	3.09	1
septacidin septacidin: structure	3.52	2
kt 6149 KW 2149: derivative of mitomycin C; structure in first source	3.09	1
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.	3.09	1	secondary alpha-hydroxy ketone; tetracyclic diterpenoid	antimalarial; antineoplastic agent; photosensitizing agent
dx 8951 [no description available]	3.09	1	pyranoindolizinoquinoline
dihydropyridines Dihydropyridines: Pyridine moieties which are partially saturated by the addition of two hydrogen atoms in any position.	2	1
carboplatin [no description available]	2	1
azidopine azidopine: structure given in first source	2	1	benzamides
brefeldin a [no description available]	2	1	macrolide antibiotic	Penicillium metabolite
staurosporine staurosporinium : Conjugate acid of staurosporine.	3.09	1	ammonium ion derivative
nb 506 NB 506: an indolocarbazole antitumor agent; structure given in first source; a DNA topoisomerase I inhibitor	3.09	1
4,4-difluoro-4-bora-3a,4a-diaza-s-indacene [no description available]	2	1	BODIPY compound
digitonin Digitonin: A glycoside obtained from Digitalis purpurea; the aglycone is digitogenin which is bound to five sugars. Digitonin solubilizes lipids, especially in membranes and is used as a tool in cellular biochemistry, and reagent for precipitating cholesterol. It has no cardiac effects.. digitonin : A spirostanyl glycoside that is digitogenin in which the 3-hydroxy group is substituted by a beta-D-glucopyranosyl-(1->3)-beta-D-galactopyranosyl-(1->2)-[beta-D-xylopyranosyl-(1->3)]-beta-D-glucopyranosyl-(1->4)-beta-D-galactopyranosyl group. It is a steroidal saponin isolated from the foxglove plant, Digitalis purpurea. It is used extensively as a mild non-ionic detergent for extracting proteins from membranes for structure and function studies.	1.98	1

Condition	Relationship Strength	Studies	Trials
Kahler Disease [description not available]	2.06	1	0
Multiple Myeloma A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.	2.06	1	0
Benign Neoplasms [description not available]	5.5	4	4
Nerve Pain [description not available]	3.46	1	1
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.	5.5	4	4
Neuralgia Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.	3.46	1	1
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	2.01	1	0
Experimental Neoplasms [description not available]	3.6	3	0
B-Cell Chronic Lymphocytic Leukemia [description not available]	2.01	1	0
Leukemia, Lymphocytic, Chronic, B-Cell A chronic leukemia characterized by abnormal B-lymphocytes and often generalized lymphadenopathy. In patients presenting predominately with blood and bone marrow involvement it is called chronic lymphocytic leukemia (CLL); in those predominately with enlarged lymph nodes it is called small lymphocytic lymphoma. These terms represent spectrums of the same disease.	2.01	1	0
Allodynia [description not available]	2.01	1	0
Ache [description not available]	2.41	2	0
Peripheral Nerve Diseases [description not available]	2.41	2	0
Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.	2.41	2	0
Peripheral Nervous System Diseases Diseases of the peripheral nerves external to the brain and spinal cord, which includes diseases of the nerve roots, ganglia, plexi, autonomic nerves, sensory nerves, and motor nerves.	2.41	2	0
Weight Gain Increase in BODY WEIGHT over existing weight.	2.01	1	0
Lassitude [description not available]	3.4	1	1
Anticipatory Vomiting [description not available]	3.4	1	1
Fatigue The state of weariness following a period of exertion, mental or physical, characterized by a decreased capacity for work and reduced efficiency to respond to stimuli.	3.4	1	1
Nausea An unpleasant sensation in the stomach usually accompanied by the urge to vomit. Common causes are early pregnancy, sea and motion sickness, emotional stress, intense pain, food poisoning, and various enteroviruses.	3.4	1	1
Local Neoplasm Recurrence [description not available]	3.4	1	1
Carcinoma, Oat Cell [description not available]	1.98	1	0
Adenocarcinoma, Basal Cell [description not available]	1.98	1	0
Cancer of Lung [description not available]	4.29	4	0
Adenocarcinoma A malignant epithelial tumor with a glandular organization.	1.98	1	0
Lung Neoplasms Tumors or cancer of the LUNG.	4.29	4	0
Carcinoma, Small Cell An anaplastic, highly malignant, and usually bronchogenic carcinoma composed of small ovoid cells with scanty neoplasm. It is characterized by a dominant, deeply basophilic nucleus, and absent or indistinct nucleoli. (From Stedman, 25th ed; Holland et al., Cancer Medicine, 3d ed, p1286-7)	1.98	1	0
Cancer of Colon [description not available]	3.82	4	0
Cancer of Liver [description not available]	1.99	1	0
Colonic Neoplasms Tumors or cancer of the COLON.	3.82	4	0
Liver Neoplasms Tumors or cancer of the LIVER.	1.99	1	0
Breast Cancer [description not available]	3.32	2	0
Cancer of Stomach [description not available]	3.32	2	0
Breast Neoplasms Tumors or cancer of the human BREAST.	3.32	2	0
Stomach Neoplasms Tumors or cancer of the STOMACH.	3.32	2	0
Carcinoma, Non-Small Cell Lung [description not available]	3.32	2	0
Carcinoma, Non-Small-Cell Lung A heterogeneous aggregate of at least three distinct histological types of lung cancer, including SQUAMOUS CELL CARCINOMA; ADENOCARCINOMA; and LARGE CELL CARCINOMA. They are dealt with collectively because of their shared treatment strategy.	3.32	2	0
Acute Liver Injury, Drug-Induced [description not available]	2	1	0
Chemical and Drug Induced Liver Injury A spectrum of clinical liver diseases ranging from mild biochemical abnormalities to ACUTE LIVER FAILURE, caused by drugs, drug metabolites, herbal and dietary supplements and chemicals from the environment.	2	1	0
Granulocytic Leukemia [description not available]	2	1	0
Leukemia, Myeloid Form of leukemia characterized by an uncontrolled proliferation of the myeloid lineage and their precursors (MYELOID PROGENITOR CELLS) in the bone marrow and other sites.	2	1	0
Lesion of Sciatic Nerve [description not available]	2	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2	1	0

krn 5500

Description

Cross-References

Synonyms (14)

Research Excerpts

Toxicity

Pharmacokinetics

Bioassays (1)

Research

Studies (26)

Study Types

Clinical Trials (3)

Trial Overview

krn 5500

Description

Cross-References

Synonyms (14)

Research Excerpts

Toxicity

Pharmacokinetics

Bioassays (1)

Research

Studies (26)

Study Types

Clinical Trials (3)

Trial Overview

Related Drugs (21)

Related Conditions (43)