Everolimus
Everolimus is an immunosuppressant that blocks growth factor-mediated proliferation of haematopoietic and nonhaematopoietic cells. Oral everolimus 0.75 or 1.5mg twice daily significantly reduced the incidence of the primary composite endpoint, efficacy failure 6 months after transplantation, compare...
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| Veröffentlicht in: | Drugs (New York, N.Y.) N.Y.), 2004-01, Vol.64 (8), p.861-872 |
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| creator | Chapman, Therese M Perry, Caroline M |
| description | Everolimus is an immunosuppressant that blocks growth factor-mediated proliferation of haematopoietic and nonhaematopoietic cells. Oral everolimus 0.75 or 1.5mg twice daily significantly reduced the incidence of the primary composite endpoint, efficacy failure 6 months after transplantation, compared with azathioprine 1-3 mg/kg/day, in adult cardiac transplant recipients. All patients also received baseline immunosuppression with cyclosporin and corticosteroids. The incidence of efficacy failure remained significantly lower in everolimus recipients than in those receiving azathioprine 1 and 2 years after cardiac transplantation. However, graft and patient survival rates at 1 year were similar in patients receiving everolimus or azathioprine. The incidence of graft vasculopathy 2 years after transplantation was significantly lower in cardiac transplant recipients receiving everolimus 0.75 mg twice daily than in those receiving azathioprine. The combined incidence of biopsy-confirmed acute rejection, graft loss, death, or loss to follow-up was similar in adult patients receiving everolimus 1.5 or 3 mg/day or mycophenolate mofetil (MMF) 2 g/day 1 or 3 years after renal transplantation. Patients also received baseline immunosuppression with cyclosporin and corticosteroids. Compared with azathioprine and MMF, everolimus is associated with a lower incidence of cytomegalovirus infection in cardiac and renal transplant recipients. Everolimus has been associated with thrombocytopenia, leucopenia and elevated serum lipids and creatinine. |
| doi_str_mv | 10.2165/00003495-200464080-00005 |
| format | Article |
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Oral everolimus 0.75 or 1.5mg twice daily significantly reduced the incidence of the primary composite endpoint, efficacy failure 6 months after transplantation, compared with azathioprine 1-3 mg/kg/day, in adult cardiac transplant recipients. All patients also received baseline immunosuppression with cyclosporin and corticosteroids. The incidence of efficacy failure remained significantly lower in everolimus recipients than in those receiving azathioprine 1 and 2 years after cardiac transplantation. However, graft and patient survival rates at 1 year were similar in patients receiving everolimus or azathioprine. The incidence of graft vasculopathy 2 years after transplantation was significantly lower in cardiac transplant recipients receiving everolimus 0.75 mg twice daily than in those receiving azathioprine. The combined incidence of biopsy-confirmed acute rejection, graft loss, death, or loss to follow-up was similar in adult patients receiving everolimus 1.5 or 3 mg/day or mycophenolate mofetil (MMF) 2 g/day 1 or 3 years after renal transplantation. Patients also received baseline immunosuppression with cyclosporin and corticosteroids. Compared with azathioprine and MMF, everolimus is associated with a lower incidence of cytomegalovirus infection in cardiac and renal transplant recipients. Everolimus has been associated with thrombocytopenia, leucopenia and elevated serum lipids and creatinine.</description><identifier>ISSN: 0012-6667</identifier><identifier>DOI: 10.2165/00003495-200464080-00005</identifier><identifier>PMID: 15059040</identifier><language>eng</language><publisher>New Zealand: Wolters Kluwer Health, Inc</publisher><subject>Administration, Oral ; Animals ; Area Under Curve ; Chronic Disease ; Disease Models, Animal ; Double-Blind Method ; Drug Administration Schedule ; Everolimus ; Graft Rejection - drug therapy ; Half-Life ; Humans ; Immunosuppressive Agents - administration & dosage ; Immunosuppressive Agents - pharmacokinetics ; Immunosuppressive Agents - therapeutic use ; Inactivation, Metabolic - genetics ; Multicenter Studies as Topic ; Organ Transplantation - adverse effects ; Organ Transplantation - pathology ; Randomized Controlled Trials as Topic ; Rats ; Ribosomal Protein S6 Kinases, 70-kDa - antagonists & inhibitors ; Ribosomal Protein S6 Kinases, 70-kDa - pharmacology ; Ribosomal Protein S6 Kinases, 70-kDa - therapeutic use ; Sirolimus - administration & dosage ; Sirolimus - analogs & derivatives ; Sirolimus - pharmacokinetics ; Sirolimus - therapeutic use ; Swine ; Time Factors ; Treatment Outcome</subject><ispartof>Drugs (New York, N.Y.), 2004-01, Vol.64 (8), p.861-872</ispartof><rights>COPYRIGHT 2004 Wolters Kluwer Health, Inc.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c378t-fa26cf219135c1a0708b3c4896b9d9aac2ee62d5f1c92382cda4d16519390d4f3</citedby><cites>FETCH-LOGICAL-c378t-fa26cf219135c1a0708b3c4896b9d9aac2ee62d5f1c92382cda4d16519390d4f3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27901,27902</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/15059040$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Chapman, Therese M</creatorcontrib><creatorcontrib>Perry, Caroline M</creatorcontrib><title>Everolimus</title><title>Drugs (New York, N.Y.)</title><addtitle>Drugs</addtitle><description>Everolimus is an immunosuppressant that blocks growth factor-mediated proliferation of haematopoietic and nonhaematopoietic cells. Oral everolimus 0.75 or 1.5mg twice daily significantly reduced the incidence of the primary composite endpoint, efficacy failure 6 months after transplantation, compared with azathioprine 1-3 mg/kg/day, in adult cardiac transplant recipients. All patients also received baseline immunosuppression with cyclosporin and corticosteroids. The incidence of efficacy failure remained significantly lower in everolimus recipients than in those receiving azathioprine 1 and 2 years after cardiac transplantation. However, graft and patient survival rates at 1 year were similar in patients receiving everolimus or azathioprine. The incidence of graft vasculopathy 2 years after transplantation was significantly lower in cardiac transplant recipients receiving everolimus 0.75 mg twice daily than in those receiving azathioprine. The combined incidence of biopsy-confirmed acute rejection, graft loss, death, or loss to follow-up was similar in adult patients receiving everolimus 1.5 or 3 mg/day or mycophenolate mofetil (MMF) 2 g/day 1 or 3 years after renal transplantation. Patients also received baseline immunosuppression with cyclosporin and corticosteroids. Compared with azathioprine and MMF, everolimus is associated with a lower incidence of cytomegalovirus infection in cardiac and renal transplant recipients. Everolimus has been associated with thrombocytopenia, leucopenia and elevated serum lipids and creatinine.</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Area Under Curve</subject><subject>Chronic Disease</subject><subject>Disease Models, Animal</subject><subject>Double-Blind Method</subject><subject>Drug Administration Schedule</subject><subject>Everolimus</subject><subject>Graft Rejection - drug therapy</subject><subject>Half-Life</subject><subject>Humans</subject><subject>Immunosuppressive Agents - administration & dosage</subject><subject>Immunosuppressive Agents - pharmacokinetics</subject><subject>Immunosuppressive Agents - therapeutic use</subject><subject>Inactivation, Metabolic - genetics</subject><subject>Multicenter Studies as Topic</subject><subject>Organ Transplantation - adverse effects</subject><subject>Organ Transplantation - pathology</subject><subject>Randomized Controlled Trials as Topic</subject><subject>Rats</subject><subject>Ribosomal Protein S6 Kinases, 70-kDa - antagonists & inhibitors</subject><subject>Ribosomal Protein S6 Kinases, 70-kDa - pharmacology</subject><subject>Ribosomal Protein S6 Kinases, 70-kDa - therapeutic use</subject><subject>Sirolimus - administration & dosage</subject><subject>Sirolimus - analogs & derivatives</subject><subject>Sirolimus - pharmacokinetics</subject><subject>Sirolimus - therapeutic use</subject><subject>Swine</subject><subject>Time Factors</subject><subject>Treatment Outcome</subject><issn>0012-6667</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2004</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNptkE1LAzEQhnNQ7If-BRE8p04-NzmWUq1Q8KLnkM2HRHa7ZdMK_nuzblUEZw7DvMwzzLwI3RBYUCLFHZRgXAtMAbjkoAAPkjhDUwBCsZSymqBZzm9Dq4W-QBMiQGjgMEWz9Xvouya1x3yJzqNtcrg61Tl6uV8_rzZ4-_TwuFpusWOVOuBoqXSREk2YcMRCBapmjista-21tY6GIKkXkThNmaLOW-7LoUQzDZ5HNke3495X2wSTdrE79Na1KTuzLD8IkIqrMrX4Z6qkD21y3S7EVPQ_gBoB13c59yGafZ9a238YAmZwynw7ZX6c-pJEQa9HdH-s2-B_wZNN7BM_y2G8</recordid><startdate>20040101</startdate><enddate>20040101</enddate><creator>Chapman, Therese M</creator><creator>Perry, Caroline M</creator><general>Wolters Kluwer Health, Inc</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope></search><sort><creationdate>20040101</creationdate><title>Everolimus</title><author>Chapman, Therese M ; Perry, Caroline M</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c378t-fa26cf219135c1a0708b3c4896b9d9aac2ee62d5f1c92382cda4d16519390d4f3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2004</creationdate><topic>Administration, Oral</topic><topic>Animals</topic><topic>Area Under Curve</topic><topic>Chronic Disease</topic><topic>Disease Models, Animal</topic><topic>Double-Blind Method</topic><topic>Drug Administration Schedule</topic><topic>Everolimus</topic><topic>Graft Rejection - drug therapy</topic><topic>Half-Life</topic><topic>Humans</topic><topic>Immunosuppressive Agents - administration & dosage</topic><topic>Immunosuppressive Agents - pharmacokinetics</topic><topic>Immunosuppressive Agents - therapeutic use</topic><topic>Inactivation, Metabolic - genetics</topic><topic>Multicenter Studies as Topic</topic><topic>Organ Transplantation - adverse effects</topic><topic>Organ Transplantation - pathology</topic><topic>Randomized Controlled Trials as Topic</topic><topic>Rats</topic><topic>Ribosomal Protein S6 Kinases, 70-kDa - antagonists & inhibitors</topic><topic>Ribosomal Protein S6 Kinases, 70-kDa - pharmacology</topic><topic>Ribosomal Protein S6 Kinases, 70-kDa - therapeutic use</topic><topic>Sirolimus - administration & dosage</topic><topic>Sirolimus - analogs & derivatives</topic><topic>Sirolimus - pharmacokinetics</topic><topic>Sirolimus - therapeutic use</topic><topic>Swine</topic><topic>Time Factors</topic><topic>Treatment Outcome</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Chapman, Therese M</creatorcontrib><creatorcontrib>Perry, Caroline M</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><jtitle>Drugs (New York, N.Y.)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Chapman, Therese M</au><au>Perry, Caroline M</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Everolimus</atitle><jtitle>Drugs (New York, N.Y.)</jtitle><addtitle>Drugs</addtitle><date>2004-01-01</date><risdate>2004</risdate><volume>64</volume><issue>8</issue><spage>861</spage><epage>872</epage><pages>861-872</pages><issn>0012-6667</issn><abstract>Everolimus is an immunosuppressant that blocks growth factor-mediated proliferation of haematopoietic and nonhaematopoietic cells. Oral everolimus 0.75 or 1.5mg twice daily significantly reduced the incidence of the primary composite endpoint, efficacy failure 6 months after transplantation, compared with azathioprine 1-3 mg/kg/day, in adult cardiac transplant recipients. All patients also received baseline immunosuppression with cyclosporin and corticosteroids. The incidence of efficacy failure remained significantly lower in everolimus recipients than in those receiving azathioprine 1 and 2 years after cardiac transplantation. However, graft and patient survival rates at 1 year were similar in patients receiving everolimus or azathioprine. The incidence of graft vasculopathy 2 years after transplantation was significantly lower in cardiac transplant recipients receiving everolimus 0.75 mg twice daily than in those receiving azathioprine. The combined incidence of biopsy-confirmed acute rejection, graft loss, death, or loss to follow-up was similar in adult patients receiving everolimus 1.5 or 3 mg/day or mycophenolate mofetil (MMF) 2 g/day 1 or 3 years after renal transplantation. Patients also received baseline immunosuppression with cyclosporin and corticosteroids. Compared with azathioprine and MMF, everolimus is associated with a lower incidence of cytomegalovirus infection in cardiac and renal transplant recipients. Everolimus has been associated with thrombocytopenia, leucopenia and elevated serum lipids and creatinine.</abstract><cop>New Zealand</cop><pub>Wolters Kluwer Health, Inc</pub><pmid>15059040</pmid><doi>10.2165/00003495-200464080-00005</doi><tpages>12</tpages></addata></record> |
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| identifier | ISSN: 0012-6667 |
| ispartof | Drugs (New York, N.Y.), 2004-01, Vol.64 (8), p.861-872 |
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| language | eng |
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| source | MEDLINE; Springer Nature - Complete Springer Journals |
| subjects | Administration, Oral Animals Area Under Curve Chronic Disease Disease Models, Animal Double-Blind Method Drug Administration Schedule Everolimus Graft Rejection - drug therapy Half-Life Humans Immunosuppressive Agents - administration & dosage Immunosuppressive Agents - pharmacokinetics Immunosuppressive Agents - therapeutic use Inactivation, Metabolic - genetics Multicenter Studies as Topic Organ Transplantation - adverse effects Organ Transplantation - pathology Randomized Controlled Trials as Topic Rats Ribosomal Protein S6 Kinases, 70-kDa - antagonists & inhibitors Ribosomal Protein S6 Kinases, 70-kDa - pharmacology Ribosomal Protein S6 Kinases, 70-kDa - therapeutic use Sirolimus - administration & dosage Sirolimus - analogs & derivatives Sirolimus - pharmacokinetics Sirolimus - therapeutic use Swine Time Factors Treatment Outcome |
| title | Everolimus |
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