{"id":"https://openalex.org/W2189443273","doi":null,"title":"Formulation modifications of PD 0313052, a direct Factor Xa Inhibitor, alter pharmacokinetics and pharma-codynamics following subcutaneous administration to rabbits.","display_name":"Formulation modifications of PD 0313052, a direct Factor Xa Inhibitor, alter pharmacokinetics and pharma-codynamics following subcutaneous administration to rabbits.","publication_year":2006,"publication_date":"2006-01-01","ids":{"openalex":"https://openalex.org/W2189443273","mag":"2189443273","pmid":"https://pubmed.ncbi.nlm.nih.gov/16959183"},"language":"en","primary_location":{"id":"pmid:16959183","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/16959183","pdf_url":null,"source":{"id":"https://openalex.org/S4306525036","display_name":"PubMed","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I1299303238","host_organization_name":"National Institutes of Health","host_organization_lineage":["https://openalex.org/I1299303238"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques","raw_type":"Journal Article"},"volume":null,"type":"article","is_traditional":true,"indexed_in":["pubmed"],"open_access":{"is_oa":false,"oa_status":"closed","oa_url":null,"any_repository_has_fulltext":false},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5067100829","display_name":"Yun-Wen Peng","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I180857899","display_name":"Pfizer (United States)","ror":"https://ror.org/01xdqrp08","country_code":"US","type":"company","lineage":["https://openalex.org/I180857899"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Yun-Wen Peng","raw_affiliation_strings":["Cardiovascular Biology, Pharmacokinetics Dynamics and Metabolism, Biostatistics, Antibacterial Biology, Pfizer Global R&D, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, Michigan 48105, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Cardiovascular Biology, Pharmacokinetics Dynamics and Metabolism, Biostatistics, Antibacterial Biology, Pfizer Global R&D, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, Michigan 48105, USA","institution_ids":["https://openalex.org/I180857899"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5111425859","display_name":"Liguo Chi","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Liguo Chi","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5108542262","display_name":"Glenn Gibson","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Glenn Gibson","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5059472639","display_name":"Nancy Janiczek","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Nancy Janiczek","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5113420487","display_name":"Paul L. Juneau","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Paul Juneau","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5056374554","display_name":"Daniel Ross","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Daniel Ross","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5032307649","display_name":"Lisa A. Perrin","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Lisa A Perrin","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"last","author":{"id":"https://openalex.org/A5106036691","display_name":"Robert J. Leadley","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I180857899","display_name":"Pfizer (United States)","ror":"https://ror.org/01xdqrp08","country_code":"US","type":"company","lineage":["https://openalex.org/I180857899"]},{"id":"https://openalex.org/I189718659","display_name":"Pfizer (United Kingdom)","ror":"https://ror.org/04x4v8p40","country_code":"GB","type":"company","lineage":["https://openalex.org/I180857899","https://openalex.org/I189718659"]}],"countries":["GB","US"],"is_corresponding":false,"raw_author_name":"Robert Leadley","raw_affiliation_strings":["Pfizer,"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Pfizer,","institution_ids":["https://openalex.org/I180857899","https://openalex.org/I189718659"]}]}],"institutions":[],"countries_distinct_count":2,"institutions_distinct_count":2,"corresponding_author_ids":[],"corresponding_institution_ids":[],"apc_list":null,"apc_paid":null,"fwci":0.0,"has_fulltext":false,"cited_by_count":0,"citation_normalized_percentile":{"value":0.18837624,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":null,"biblio":{"volume":"9","issue":"2","first_page":"140","last_page":"8"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T10881","display_name":"Blood Coagulation and Thrombosis Mechanisms","score":0.9473000168800354,"subfield":{"id":"https://openalex.org/subfields/2720","display_name":"Hematology"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}},"topics":[{"id":"https://openalex.org/T10881","display_name":"Blood Coagulation and Thrombosis Mechanisms","score":0.9473000168800354,"subfield":{"id":"https://openalex.org/subfields/2720","display_name":"Hematology"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}},{"id":"https://openalex.org/T10285","display_name":"Venous Thromboembolism Diagnosis and Management","score":0.007000000216066837,"subfield":{"id":"https://openalex.org/subfields/2724","display_name":"Internal Medicine"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}},{"id":"https://openalex.org/T11280","display_name":"Hemophilia Treatment and Research","score":0.004699999932199717,"subfield":{"id":"https://openalex.org/subfields/2720","display_name":"Hematology"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}}],"keywords":[{"id":"https://openalex.org/keywords/factor-xa-inhibitors","display_name":"factor Xa inhibitors","score":0.8539999723434448},{"id":"https://openalex.org/keywords/subcutaneous-administration","display_name":"subcutaneous administration","score":0.875},{"id":"https://openalex.org/keywords/pharmaceutical-formulations","display_name":"drug formulation","score":0.8650000095367432},{"id":"https://openalex.org/keywords/pharmacokinetics","display_name":"pharmacokinetics","score":0.9850000143051147},{"id":"https://openalex.org/keywords/pharmacodynamics","display_name":"pharmacodynamics","score":0.9980000257492065},{"id":"https://openalex.org/keywords/antithrombotic-agents","display_name":"antithrombotic agents","score":0.8579999804496765},{"id":"https://openalex.org/keywords/plasma-drug-concentration","display_name":"plasma drug concentration","score":0.4699999988079071},{"id":"https://openalex.org/keywords/factor-xa-activity","display_name":"factor Xa activity","score":0.7860000133514404},{"id":"https://openalex.org/keywords/prothrombin-time","display_name":"prothrombin time","score":0.9179999828338623},{"id":"https://openalex.org/keywords/sesame-oil","display_name":"sesame oil","score":0.781000018119812},{"id":"https://openalex.org/keywords/f127","display_name":"F127","score":0.9259999990463257},{"id":"https://openalex.org/keywords/methylcellulose","display_name":"methylcellulose","score":0.9359999895095825},{"id":"https://openalex.org/keywords/rabbits","display_name":"rabbits","score":0.5170000195503235}],"concepts":[{"id":"https://openalex.org/C112705442","wikidata":"https://www.wikidata.org/wiki/Q323936","display_name":"Pharmacokinetics","level":2,"score":0.7445177435874939},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.6662412881851196},{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.6613216400146484},{"id":"https://openalex.org/C181389837","wikidata":"https://www.wikidata.org/wiki/Q461809","display_name":"Bioavailability","level":2,"score":0.6169813275337219},{"id":"https://openalex.org/C111113717","wikidata":"https://www.wikidata.org/wiki/Q725307","display_name":"Pharmacodynamics","level":3,"score":0.5642691850662231},{"id":"https://openalex.org/C2777015399","wikidata":"https://www.wikidata.org/wiki/Q4775337","display_name":"Antithrombotic","level":2,"score":0.5320450067520142},{"id":"https://openalex.org/C2778382381","wikidata":"https://www.wikidata.org/wiki/Q179217","display_name":"Coagulation","level":2,"score":0.5273528695106506},{"id":"https://openalex.org/C2777397205","wikidata":"https://www.wikidata.org/wiki/Q275792","display_name":"Saline","level":2,"score":0.47213512659072876},{"id":"https://openalex.org/C2780434524","wikidata":"https://www.wikidata.org/wiki/Q1144385","display_name":"Prothrombin time","level":2,"score":0.4357258975505829},{"id":"https://openalex.org/C71924100","wikidata":"https://www.wikidata.org/wiki/Q11190","display_name":"Medicine","level":0,"score":0.2538370192050934},{"id":"https://openalex.org/C42219234","wikidata":"https://www.wikidata.org/wiki/Q131130","display_name":"Anesthesia","level":1,"score":0.14174333214759827},{"id":"https://openalex.org/C126322002","wikidata":"https://www.wikidata.org/wiki/Q11180","display_name":"Internal medicine","level":1,"score":0.09359738230705261}],"mesh":[{"descriptor_ui":"D000818","descriptor_name":"Animals","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D000990","descriptor_name":"Antithrombin III","qualifier_ui":"Q000008","qualifier_name":"administration & dosage","is_major_topic":false},{"descriptor_ui":"D000990","descriptor_name":"Antithrombin III","qualifier_ui":"Q000493","qualifier_name":"pharmacokinetics","is_major_topic":true},{"descriptor_ui":"D000990","descriptor_name":"Antithrombin III","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D002626","descriptor_name":"Chemistry, Pharmaceutical","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D004305","descriptor_name":"Dose-Response Relationship, Drug","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D005260","descriptor_name":"Female","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D005343","descriptor_name":"Fibrinolytic Agents","qualifier_ui":"Q000008","qualifier_name":"administration & dosage","is_major_topic":false},{"descriptor_ui":"D005343","descriptor_name":"Fibrinolytic Agents","qualifier_ui":"Q000097","qualifier_name":"blood","is_major_topic":false},{"descriptor_ui":"D005343","descriptor_name":"Fibrinolytic Agents","qualifier_ui":"Q000493","qualifier_name":"pharmacokinetics","is_major_topic":true},{"descriptor_ui":"D005343","descriptor_name":"Fibrinolytic Agents","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D007279","descriptor_name":"Injections, Subcutaneous","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D010880","descriptor_name":"Piperidines","qualifier_ui":"Q000008","qualifier_name":"administration & dosage","is_major_topic":false},{"descriptor_ui":"D010880","descriptor_name":"Piperidines","qualifier_ui":"Q000097","qualifier_name":"blood","is_major_topic":false},{"descriptor_ui":"D010880","descriptor_name":"Piperidines","qualifier_ui":"Q000493","qualifier_name":"pharmacokinetics","is_major_topic":true},{"descriptor_ui":"D010880","descriptor_name":"Piperidines","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D011817","descriptor_name":"Rabbits","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false}],"locations_count":2,"locations":[{"id":"pmid:16959183","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/16959183","pdf_url":null,"source":{"id":"https://openalex.org/S4306525036","display_name":"PubMed","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I1299303238","host_organization_name":"National Institutes of Health","host_organization_lineage":["https://openalex.org/I1299303238"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques","raw_type":"Journal Article"},{"id":"mag:2189443273","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/16959183","pdf_url":null,"source":{"id":"https://openalex.org/S4306525036","display_name":"PubMed","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I1299303238","host_organization_name":"National Institutes of Health","host_organization_lineage":["https://openalex.org/I1299303238"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":null,"is_accepted":false,"is_published":false,"raw_source_name":"PubMed","raw_type":null}],"best_oa_location":null,"sustainable_development_goals":[{"score":0.9537000060081482,"id":"https://metadata.un.org/sdg/3","display_name":"Good health and well-being"}],"study_designs":[],"awards":[],"funders":[],"has_content":{"pdf":false,"grobid_xml":false},"content_urls":null,"referenced_works_count":30,"referenced_works":["https://openalex.org/W1973274232","https://openalex.org/W1988590460","https://openalex.org/W1990199384","https://openalex.org/W2002128115","https://openalex.org/W2005017217","https://openalex.org/W2005066506","https://openalex.org/W2005219492","https://openalex.org/W2014538668","https://openalex.org/W2016327253","https://openalex.org/W2021621876","https://openalex.org/W2021953458","https://openalex.org/W2023320697","https://openalex.org/W2026200435","https://openalex.org/W2028162842","https://openalex.org/W2033606955","https://openalex.org/W2036451082","https://openalex.org/W2057909264","https://openalex.org/W2064826963","https://openalex.org/W2080528872","https://openalex.org/W2103740849","https://openalex.org/W2106451839","https://openalex.org/W2126518073","https://openalex.org/W2144417922","https://openalex.org/W2156060448","https://openalex.org/W2160099234","https://openalex.org/W2284651264","https://openalex.org/W2405790291","https://openalex.org/W2428808398","https://openalex.org/W2463994390","https://openalex.org/W2886313703"],"related_works":["https://openalex.org/W1988590460","https://openalex.org/W2120096493","https://openalex.org/W7014560635","https://openalex.org/W2018183727","https://openalex.org/W7167275743","https://openalex.org/W1993406555","https://openalex.org/W2515763820","https://openalex.org/W2582975186","https://openalex.org/W2073040389","https://openalex.org/W2173118298"],"abstract_inverted_index":{"PURPOSE:":[0],"PD":[1,48,55,94,117,132,193,198,207,225,231,238,247,271,274,278],"0313052":[2,49,56,95,133,208,239,279],"is":[3,209,219,280],"a":[4,51,125,220,281,287],"potent,":[5],"direct":[6],"factor":[7],"Xa":[8],"(FXa)":[9],"inhibitor":[10],"(Ki":[11],"=":[12,140,146,151],"0.33":[13],"nM)":[14],"and":[15,71,83,88,102,112,136,148,155,166,176,185,216,227,246,270,276],"its":[16],"antithrombotic":[17,289],"effect":[18],"has":[19],"been":[20],"previously":[21],"demonstrated":[22],"in":[23,59,234,243],"several":[24],"animal":[25],"models,":[26],"via":[27],"intravenous":[28],"(IV)":[29],"administration.":[30],"In":[31,180],"the":[32,44,84,89,109,224,235,244,268],"present":[33],"study,":[34],"we":[35],"evaluated":[36],"four":[37],"different":[38],"subcutaneous":[39,52],"(SC)":[40],"formulations":[41,157,182,262],"to":[42,107,171,214,255,266],"test":[43],"feasibility":[45],"of":[46,91,93,116,121,183,230,237,249,273],"developing":[47],"as":[50,286],"agent.":[53,290],"METHODS:":[54],"was":[57,78,124],"formulated":[58],"saline,":[60],"methylcellulose":[61,64],"(MC,":[62],"0.5%":[63],"solution":[65],"containing":[66],"1%":[67],"Tween-80),":[68],"sesame":[69,186],"oil,":[70],"F127":[72,184],"(25%":[73],"aqueous":[74],"solution).":[75],"Each":[76],"formulation":[77,236],"injected":[79],"subcutaneously":[80],"into":[81],"rabbits":[82,215],"relative":[85],"plasma":[86,134,228],"exposure":[87],"duration":[90],"action":[92],"were":[96,105],"assessed.":[97],"Plasma":[98],"concentration,":[99],"FXa":[100,137,162],"activity,":[101,163],"coagulation":[103,164],"parameters":[104,226],"used":[106],"monitor":[108],"pharmacokinetic":[110],"(PK)":[111],"pharmacodynamic":[113],"(PD)":[114],"profiles":[115,248,272],"0313052.":[118,232],"RESULTS:":[119],"Regardless":[120],"formulation,":[122],"there":[123,218],"significant":[126],"(p":[127],"<":[128],"0.05)":[129],"correlation":[130,222],"between":[131,223],"concentration":[135],"activity":[138],"(R2":[139,145,150],"0.90),":[141],"prothrombin":[142],"time":[143],"(PT)":[144],"0.86),":[147],"Heptest":[149],"0.93).":[152],"The":[153,203],"saline":[154],"MC":[156],"had":[158],"similar":[159],"effects":[160,191,199],"on":[161,192],"parameters,":[165],"Heptest,":[167],"peaking":[168],"at":[169],"30":[170],"120":[172],"minutes":[173],"after":[174,211,252],"administration":[175,213,254],"decreasing":[177],"rapidly":[178],"thereafter.":[179],"contrast,":[181],"oil":[187],"yielded":[188],"lower":[189],"maximal":[190],"markers":[194],"but":[195],"produced":[196],"sustained":[197],"over":[200],"time.":[201],"CONCLUSION:":[202],"data":[204],"indicate":[205],"that":[206,217,260,277],"bioavailable":[210],"SC":[212,253,261,288],"strong":[221],"concentrations":[229],"Modifications":[233],"produce":[240],"marked":[241],"differences":[242],"PK":[245,269],"this":[250],"agent":[251],"rabbits.":[256],"These":[257],"results":[258],"suggest":[259],"can":[263],"be":[264],"optimized":[265],"improve":[267],"0313052,":[275],"viable":[282],"candidate":[283],"for":[284],"development":[285]},"counts_by_year":[],"updated_date":"2026-10-31T12:09:11.096373","created_date":"2016-06-24T00:00:00"}
