Sirolimus (rapamycin): From the soil of Easter Island to a bright future

Paghdal, Kapila V.; Schwartz, Robert A.

doi:10.1016/j.jaad.2007.05.021

Cited by 84 publications

(70 citation statements)

References 28 publications

(35 reference statements)

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“…Its use in preventing acute rejection after renal transplantations and in chronic allograft nephropathia is becoming increasingly common. The most frequent side effects are hyperlipidemia, thrombocytopenia, mild anemia, diarrhea, lymphocele, increase in the prevalence of inguinal herniation, and delay in wound healing (2). An increase in liver enzymes, development of acnes, interstitial pneumonia, thrombotic microangiopathy, angioedema, and eyelid edema has been reported in rare cases (5).…”

Section: Discussionmentioning

confidence: 99%

“…In connection with this, 11 to 130 weeks after the initiation of treatment, their dose ranged between 2 and 10 mg/day; 13 patients had recovered from 4 weeks up to 6 years after stopping the medication and there was no change in seven patients (2,18). No difference was observed in the patients in terms of gender, and nearly all of them were middle-aged.…”

Section: Discussionmentioning

confidence: 99%

“…Although dyslipidemia, thrombocytopenia, and lymphocele occur relatively often after sirolimus therapy, the development of lymphedema associated with sirolimus is a rare complication (2). We have more knowledge about the etiology and treatment of lymphedema that develops after breast surgery.…”

Section: Introductionmentioning

confidence: 99%

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Lymphedema Treatment in a Patient with a History of Intestinal Transplantation and Mesenchymal Stem Cell Transplantation

Donmez¹,

Kilinc²,

Doğan³

et al. 2015

Turk J Phys Med Rehab

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Lymphedema is a rare complication of sirolimus treatment in transplantation patients. We present a case of a 14-year-old female patient who developed lymphedema in three extremities. The patient had undergone ileal and colon resections after sustaining a gunshot to her abdomen. Four months after the injury, she had developed a short bowel syndrome and underwent small intestine transplantation from a cadaver and mesenchymal stem cell transplantation to prevent rejection. Because of kidney failure developed at postoperative month 3, mycophenolate mofetil therapy was discontinued and sirolimus therapy was initiated. The patient was monitored under this therapy until postoperative month 11 when she had swelling in both the legs and left arm. Her condition significantly improved with complex decongestive therapy. This is the first case in the literature involving mesenchymal stem cell transplantation together with ileum transplantation. This case is also noteworthy in terms of lymphedema treatment administered and the involvement of three extremities.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Lymphedema Treatment in a Patient with a History of Intestinal Transplantation and Mesenchymal Stem Cell Transplantation

Donmez¹,

Kilinc²,

Doğan³

et al. 2015

Turk J Phys Med Rehab

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“…RAPA showed great promise as an immunosuppressive agent in transplant recipients as well as antiproliferative and anti-angiogenic agent in a variety of solid tumor treatments. Antiproliferative effects of RAPA have been demonstrated not only on lymphocytes but also on vascular and tumor cells (Barenholz, 2001;Kakegawa et al, 2003;MacDonald et al, 2000;Paghdal & Schwartz, 2007).…”

Section: Introductionmentioning

confidence: 99%

Fusogenic pH sensitive liposomal formulation for rapamycin: Improvement of antiproliferative effect

Ghanbarzadeh

Khorrami

Khosroshahi

et al. 2014

Pharmaceutical Biology

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Context: Liposomes are increasingly employed to deliver chemotherapeutic agents, antisense oligonucleotides, and genes to various therapeutic targets. Objective: The present investigation evaluates the ability of fusogenic pH-sensitive liposomes of rapamycin in increasing its antiproliferative effect on human breast adenocarcinoma (MCF-7) cell line. Materials and methods: Cholesterol (Chol) and dipalmitoylphosphatidylcholine (DPPC) (DPPC:Chol, 7:3) were used to prepare conventional rapamycin liposomes by a modified ethanol injection method. Dioleoylphosphatidylethanolamine (DOPE) was used to produce fusogenic and pH-sensitive properties in liposomes simultaneously (DPPC:Chol:DOPE, 7:3:4.2). The prepared liposomes were characterized by their size, zeta potential, encapsulation efficiency percent (EE%), and chemical stability during 6 months. The antiproliferative effects of both types of rapamycin liposomes (10, 25, and 50 nmol/L) with optimized formulations were assessed on MCF-7 cells, as cancerous cells, and human umbilical vein endothelial cells (HUVEC), as healthy cells, employing the diphenyltetrazolium bromide (MTT) assay for 72 h. Results and discussion: The particle size, zeta potential, and EE% of the liposomes were 165 AE 12.3 and 178 AE 15.4 nm, À39.6 AE 1.3, and À41.2 AE 2.1 mV as well as 76.9 AE 2.6 and 76.9 AE 2.6% in conventional and fusogenic pH-sensitive liposomes, respectively. Physicochemical stability results indicated that both liposome types were relatively stable at 4 C than 25 C. In vitro antiproliferative evaluation showed that fusogenic pH-sensitive liposomes had better antiproliferative effects on MCF-7 cells compared to the conventional liposomes. Conversely, fusogenic pH-sensitive liposomes had less cytotoxicity on HUVEC cell line. KeywordsAntiproliferative effect, breast cancer, fusogenic pH-sensitive liposome, rapamycin History

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“…Rapamycin binds with high specificity to mTOR, and binding results in inhibition of mTOR activity and ultimately in downregulation of cell growth. [16] Rapamycin has a molecular weight of 914.2 grams/mol, allowing for its absorption through the superficial layers of the epidermis to the deep dermal layer implicated in the development of facial angiofibromas.…”

mentioning

confidence: 99%

Topical Rapamycin Therapy to Alleviate the Cutaneous Manifestations of Tuberous Sclerosis Complex

Koenig

Hebert

Roberson³

et al. 2012

Drugs R D

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Background and Objectives: Facial angiofibromas are disfiguring facial lesions, present in up to 80% of patients with tuberous sclerosis complex. Recent elucidation of the complex cell signaling pathways that are disrupted in tuberous sclerosis indicates that rapamycin may be successful in alleviating the appearance of these lesions. The objectives of the current study were to evaluate the safety of topically applied rapamycin in patients with tuberous sclerosis complex and to determine its potential effectiveness in treatment of facial angiofibromas.Patients and Methods: The study was a prospective, randomized, doubleblind, placebo-controlled study performed at the University of Texas Health Science Center at Houston. Study subjects were recruited from the patient populations at the University of Texas Tuberous Sclerosis Center of Excellence. All subjects were over the age of 13 years and had a diagnosis of

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Sirolimus (rapamycin): From the soil of Easter Island to a bright future

Cited by 84 publications

References 28 publications

Lymphedema Treatment in a Patient with a History of Intestinal Transplantation and Mesenchymal Stem Cell Transplantation

Lymphedema Treatment in a Patient with a History of Intestinal Transplantation and Mesenchymal Stem Cell Transplantation

Fusogenic pH sensitive liposomal formulation for rapamycin: Improvement of antiproliferative effect

Topical Rapamycin Therapy to Alleviate the Cutaneous Manifestations of Tuberous Sclerosis Complex

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