aprinocarsen profile

ISIS 3521: 20-nucleotide phosphorothioate antisense molecule that targets protein kinase C-alpha isoenzyme [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	121493082
MeSH ID	M0469884

Synonym
aprinocarsen [inn]
deoxyribonucleic acid, d(p-thio)(a-c-t-t-t-g-a-g-t-g-g-t-c-g-c-t-c-t-t-g)
ly900003
ly 900003
isis 3521
cgp 64128a
unii-fmt95051cq
151879-73-1
fmt95051cq ,
cgp64128a
isi641a
isi-641a
isi 641a

Excerpt	Reference
" Plasma samples were collected to assess individual steady-state concentrations and to relate this pharmacokinetic parameter to observed toxicities and responses."	( A randomized phase II and pharmacokinetic study of the antisense oligonucleotides ISIS 3521 and ISIS 5132 in patients with hormone-refractory prostate cancer. Chi, K; Dorr, A; Eisenhauer, E; Ernst, SD; Geary, RS; Hall, S; Moore, M; Reyno, L; Tolcher, AW; Venner, PM; Walsh, W, 2002)

Excerpt	Reference
" CGP 64128A in combination with adriamycin resulted in superadditive antitumor effects against BT20 human breast carcinomas with complete tumor responses, and in combination with mitomycin-C superadditive antitumor effects with cures were observed against NCI-H460 human large cell carcinomas."	( Antitumor activity of a PKC-alpha antisense oligonucleotide in combination with standard chemotherapeutic agents against various human tumors transplanted into nude mice. Dean, NM; Fabbro, D; Geiger, T; Müller, M, 1998)
"LY900003 can be administered safely in combination with cisplatin and gemcitabine and is associated with antitumor activity in patients with advanced NSCLC."	( A phase I/II study of LY900003, an antisense inhibitor of protein kinase C-alpha, in combination with cisplatin and gemcitabine in patients with advanced non-small cell lung cancer. Belt, R; Dow, E; Figueroa, JA; Geary, R; George, S; Holmlund, J; Leonardo, J; McCachren, S; Miller, GL; Modiano, M; Oliver, JW; Otterson, GA; Ritch, P; Valdivieso, M; Villalona-Calero, MA, 2004)

Excerpt	Reference
" Administration via the gastrointestinal tract gave negligible bioavailability (< 2%)."	( Pulmonary bioavailability of a phosphorothioate oligonucleotide (CGP 64128A): comparison with other delivery routes. Bayley, D; Craig, SJ; Cummins, LL; Giddings, J; Hastewell, JG; Nicklin, PL; Phillips, JA, 1998)
" The dose-dependent increase in pulmonary bioavailability suggests that low doses may be retained in the lungs for local effects whereas higher doses may be suitable for the treatment of a broader spectrum of systemic diseases."	( Pulmonary bioavailability of a phosphorothioate oligonucleotide (CGP 64128A): comparison with other delivery routes. Bayley, D; Craig, SJ; Cummins, LL; Giddings, J; Hastewell, JG; Nicklin, PL; Phillips, JA, 1998)

Excerpt	Reference
" Pulmonary delivery represents a promising mode of non-parenteral dosing for antisense oligonucleotides."	( Pulmonary bioavailability of a phosphorothioate oligonucleotide (CGP 64128A): comparison with other delivery routes. Bayley, D; Craig, SJ; Cummins, LL; Giddings, J; Hastewell, JG; Nicklin, PL; Phillips, JA, 1998)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	11 (36.67)	18.2507
2000's	19 (63.33)	29.6817
2010's	0 (0.00)	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	7 (22.58%)	5.53%
Reviews	12 (38.71%)	6.00%
Case Studies	1 (3.23%)	4.05%
Observational	0 (0.00%)	0.25%
Other	11 (35.48%)	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
bisindolylmaleimide i bisindolylmaleimide I: a bis(indolyl)maleimide	3.1	1	0
go 6976 [no description available]	3.1	1	0	indolocarbazole; organic heterohexacyclic compound	EC 2.7.11.13 (protein kinase C) inhibitor
ro 31-8220 Ro 31-8220: a protein kinase C inhibitor	3.1	1	0	imidothiocarbamic ester; indoles; maleimides	EC 2.7.11.13 (protein kinase C) inhibitor
pyrroles 1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.	3.1	1	0	pyrrole; secondary amine
deoxycytidine [no description available]	3.4	1	1	pyrimidine 2'-deoxyribonucleoside	Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
tetradecanoylphorbol acetate Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.. phorbol ester : Esters of phorbol, originally found in croton oil (from Croton tiglium, of the family Euphorbiaceae). A number of phorbol esters possess activity as tumour promoters and activate the mechanisms associated with cell growth. Some of these are used in experiments as activators of protein kinase C.. phorbol 13-acetate 12-myristate : A phorbol ester that is phorbol in which the hydroxy groups at the cyclopropane ring juction (position 13) and the adjacent carbon (position 12) have been converted into the corresponding acetate and myristate esters. It is a major active constituent of the seed oil of Croton tiglium. It has been used as a tumour promoting agent for skin carcinogenesis in rodents and is associated with increased cell proliferation of malignant cells. However its function is controversial since a decrease in cell proliferation has also been observed in several cancer cell types.	2	1	0	acetate ester; diester; phorbol ester; tertiary alpha-hydroxy ketone; tetradecanoate ester	antineoplastic agent; apoptosis inducer; carcinogenic agent; mitogen; plant metabolite; protein kinase C agonist; reactive oxygen species generator
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).	2	1	0	taxane diterpenoid; tetracyclic diterpenoid	antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent
gemcitabine gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer.	3.4	1	1	organofluorine compound; pyrimidine 2'-deoxyribonucleoside	antimetabolite; antineoplastic agent; antiviral drug; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; environmental contaminant; immunosuppressive agent; photosensitizing agent; prodrug; radiosensitizing agent; xenobiotic
7-hydroxystaurosporine [no description available]	3.11	1	0
ro 32-0432 [no description available]	3.1	1	0
ruboxistaurin ruboxistaurin: inhibits protein kinase C beta; structure in first source	3.1	1	0
ophiocordin ophiocordin: metabolite of Cordyceps ophioglossoides	3.1	1	0
staurosporine staurosporinium : Conjugate acid of staurosporine.	3.11	1	0	ammonium ion derivative
midostaurin midostaurin : An organic heterooctacyclic compound that is the N-benzoyl derivative of staurosporine.	3.11	1	0	benzamides; gamma-lactam; indolocarbazole; organic heterooctacyclic compound	antineoplastic agent; EC 2.7.11.13 (protein kinase C) inhibitor
oligonucleotides [no description available]	5.92	4	1
bryostatin 1 bryostatin 1: a protein kinase C activator; macrocyclic lactone from marine Bryozoan Bugula neritina; RN given refers to (1S-(1R,3R,5Z,7S,8E,11R,12R(2E,4E),13E,15R,17S(S),21S,23S,25R))-isomer; structure given in first source; activates protein kinase c. bryostatin 1 : A member of the class of bryostatins that is (17E)-2-oxooxacyclohexacos-17-ene which is substituted by hydroxy groups at positions 4, 10, and 20; an acetoxy group at position 8; methyl groups at positions 9, 9, 18, and 19; 2-methoxy-2-oxoethylidene groups at positions 14 and 24; an (E,E)-octa-2,4-dienoyloxy group at position 21; and with oxygen bridges linking positions 6 to 10, 12 to 16, and 20 to 24. It is one of the most abundant member of the class of bryostatins.	4.02	2	0
oblimersen oblimersen: targets the Bcl-2 oncogene good efficacy with low toxicity tumour regressions	4.31	3	0

Condition	Relationship Strength	Studies	Trials
Adenocarcinoma, Basal Cell [description not available]	3.39	1	1
Colorectal Cancer [description not available]	4.36	2	2
Adenocarcinoma A malignant epithelial tumor with a glandular organization.	3.39	1	1
Colorectal Neoplasms Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.	4.36	2	2
Metastase [description not available]	4.36	2	2
Cancer of Prostate [description not available]	3.8	2	1
Neoplasm Metastasis The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.	4.36	2	2
Prostatic Neoplasms Tumors or cancer of the PROSTATE.	3.8	2	1
Breast Cancer [description not available]	2.93	1	0
Breast Neoplasms Tumors or cancer of the human BREAST.	2.93	1	0
Carcinoma, Non-Small Cell Lung [description not available]	4.72	2	1
Cancer of Lung [description not available]	5	3	1
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.	4.72	2	1
Lung Neoplasms Tumors or cancer of the LUNG.	5	3	1
Cancer of Ovary [description not available]	3.4	1	1
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.	3.4	1	1
Benign Neoplasms [description not available]	7.7	12	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.	7.7	12	1
Pyrexia [description not available]	4.71	2	1
Bilateral Headache [description not available]	3.4	1	1
Diffuse Mixed Small and Large Cell Lymphoma [description not available]	3.4	1	1
Fever An abnormal elevation of body temperature, usually as a result of a pathologic process.	4.71	2	1
Headache The symptom of PAIN in the cranial region. It may be an isolated benign occurrence or manifestation of a wide variety of HEADACHE DISORDERS.	3.4	1	1
Lymphoma, Non-Hodgkin Any of a group of malignant tumors of lymphoid tissue that differ from HODGKIN DISEASE, being more heterogeneous with respect to malignant cell lineage, clinical course, prognosis, and therapy. The only common feature among these tumors is the absence of giant REED-STERNBERG CELLS, a characteristic of Hodgkin's disease.	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
Experimental Neoplasms [description not available]	1.99	1	0
Colitis, Granulomatous [description not available]	2.92	1	0
Crohn Disease A chronic transmural inflammation that may involve any part of the DIGESTIVE TRACT from MOUTH to ANUS, mostly found in the ILEUM, the CECUM, and the COLON. In Crohn disease, the inflammation, extending through the intestinal wall from the MUCOSA to the serosa, is characteristically asymmetric and segmental. Epithelioid GRANULOMAS may be seen in some patients.	2.92	1	0
Vascular Diseases Pathological processes involving any of the BLOOD VESSELS in the cardiac or peripheral circulation. They include diseases of ARTERIES; VEINS; and rest of the vasculature system in the body.	2.92	1	0
Coagulation Disorders, Blood [description not available]	2.91	1	0
Lassitude [description not available]	2.91	1	0
Thrombopenia [description not available]	2.91	1	0
Blood Coagulation Disorders Hemorrhagic and thrombotic disorders that occur as a consequence of abnormalities in blood coagulation due to a variety of factors such as COAGULATION PROTEIN DISORDERS; BLOOD PLATELET DISORDERS; BLOOD PROTEIN DISORDERS or nutritional conditions.	2.91	1	0
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.	2.91	1	0
Thrombocytopenia A subnormal level of BLOOD PLATELETS.	2.91	1	0
Blood Diseases [description not available]	2	1	0
Hematologic Diseases Disorders of the blood and blood forming tissues.	2	1	0
Bladder Cancer [description not available]	2	1	0
Urinary Bladder Neoplasms Tumors or cancer of the URINARY BLADDER.	2	1	0

aprinocarsen

Description

Cross-References

Synonyms (13)

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Research

Studies (30)

Study Types

aprinocarsen

Description

Cross-References

Synonyms (13)

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Research

Studies (30)

Study Types

Related Drugs (17)

Related Conditions (39)