Delving into the Latest Updates on Megestrol Acetate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

17-Acetoxy-6-methylpregna-4,6-diene-3,20-dione, 17-Hydroxy-6-methylpregna-4,6-diene-3,20-dione 17-acetate, 17alpha-Acetoxy-6-dehydro-6-methylprogesterone

+ [37]

Target

PR

Mechanism

PR agonists(Progesterone receptor agonists)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesUrogenital Diseases

Active Indication

Acquired Immunodeficiency Syndrome

Inactive Indication

AnorexiaCachexiaDementia+ [4]

Originator Organization

Bristol Myers Squibb Co.

Active Organization

Endo Operations Ltd.

Inactive Organization

Par Pharmaceutical, Inc.Endo Pharmaceuticals, Inc.

Bristol Myers Squibb Co.

+ [2]

Drug Highest PhaseApproved

First Approval Date

US (18 Aug 1971),

Acquired Immunodeficiency Syndrome

RegulationOrphan Drug (EU)

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Structure

Molecular FormulaC24H32O4

InChIKeyRQZAXGRLVPAYTJ-GQFGMJRRSA-N

CAS Registry595-33-5

OBJECTIVETo evaluate the disease course of patients with low grade endometrial stromal sarcoma (LG-ESS) and compare oncologic outcomes associated with hormonal therapy in primary and recurrent disease.METHODSThis is a retrospective study of patients with LG-ESS who underwent active treatment between January 2000 and July 2023. Recurrence-free survival (RFS) and overall survival (OS) were estimated using the Kaplan-Meier product-limit estimator and modeled via Cox proportional hazards regression.RESULTSA total of 221 patients were included; 58 % of patients (91/157) were stage I, 12 % (19/157) stage II, 13 % (20/157) stage III, and 17 % (27/157) stage IV. Surgery was the primary treatment for 98 % (213/218). Only 79 patients received hormonal adjuvant therapy, 58 % (46/79) Megace, 24 % (19/79) Letrozole, and 18 % (14/79) received other hormonal therapy. There was no significant difference in RFS (p = 0.159) and OS (p = 0.167) between patients receiving Megace versus Letrozole as adjuvant therapy. At first recurrence, patients given Megace had a similar RFS to those on Letrozole (p = 0.302), but a better OS (27 vs 10 months, p = 0.018). Negative status of estrogen, smooth muscle actin, and desmin were associated with lower RFS (p = 0.039, p = 0.002, and p = 0.015, respectively) and OS (p = 0.008, p = 0.012, and p = 0.013, respectively). Lymphovascular invasion was associated with lower RFS (p = 0.033), and negative status of progesterone was associated with lower OS (p = 0.003).CONCLUSIONThere was no difference in oncologic outcomes between Megace and Letrozole in patients who received adjuvant therapy for LG-ESS. Megace may have potential survival advantage in recurrent disease. Further study is warranted to determine the most effective agents and their sequence in the treatment of LG-ESS.

01 Nov 2024·Immunity, Inflammation and Disease

Identification of Vesicle‐Mediated Transport‐Related Genes for Predicting Prognosis, Immunotherapy Response, and Drug Screening in Cervical Cancer

Article

Author: Lv, Hongqing ; Zhang, Lin ; Lou, Shuai

ABSTRACTBackgroundCervical cancer is one of the most common malignancies among women. Vesicle‐mediated transport mechanisms significantly influence tumor cell behavior through intercellular material exchange. However, prognostic significance in CC patients remains underexplored.Research Design and MethodsWe identified differentially expressed vesicle‐mediated transport‐related genes from TCGA and GeneCards datasets through differential expression analysis. We constructed a prognostic model using Cox regression and LASSO regression, categorized patients into high‐ and low‐risk groups, and validated the model in the GEO data set. A nomogram integrating clinical features and risk scores demonstrated the model's independent prognostic capability. We analyzed tumor immune cell infiltration, immune checkpoints, and predicted immunotherapy responses in the high‐ and low‐risk groups. Finally, we screened potential drugs for targeting CC and conducted drug‐sensitivity analysis.ResultsWe successfully established a 10‐gene prognostic model based on VMTRGs. The low‐risk group exhibited favorable prognosis, significant immune cell infiltration, and promising immunotherapy response, whereas the high‐risk group showed higher sensitivity to chemotherapeutic agents such as Docetaxel and Paclitaxel. Potential drugs identified for targeting CC patients included Megestrol acetate, Lenvatinib, Adavosertib, and Barasertib.ConclusionsThe VMTRG‐based prognostic model demonstrates reliable clinical prognostic value and enhances understanding of vesicle‐mediated transport mechanisms in CC.

01 Nov 2024·Journal of the American Pharmacists Association

Megesterol acetate as an overlooked cause of hyperglycemia in end-stage renal disease: A case of polypharmacy

Article

Author: Aurora, John ; Fortunati, Julieta Rossi ; Erenler, Feyza ; Zheng, Theresa

OBJECTIVESThis case report highlights an overlooked cause of hyperglycemia and risk of polypharmacy in a patient with end-stage renal disease (ESRD).CASE SUMMARYA 75-year-old non-English speaking male with T2DM, hypertension, coronary artery disease status post percutaneous coronary intervention, and ESRD secondary to IgG Kappa nephropathy on nightly peritoneal dialysis reported a loss of appetite, decrease in weight, and an increase in symptoms of depression. As a result of these symptoms, his nephrologist initiated megestrol acetate (MA), an agent commonly used in ESRD to help stimulate appetite and improve weight. After starting MA, his blood glucose (BG) significantly worsened, due to its glucocorticoid properties. Basal insulin was started to manage his hyperglycemia, but there was minimal improvement in BG. As the patient was referred to the endocrinology clinical pharmacist for diabetes management, it was identified that his weight loss began after starting dulaglutide, which led to a weight loss of 11 kg (12.9%). The Naranjo algorithm was used, and he had a score of 6, which is a probable reaction. The patient's endocrinology and nephrology teams agreed to discontinue MA and dulaglutide as they resulted in opposing effects on appetite and BG, as well as insulin glargine. The patient's BG was tightly controlled off MA and his appetite, weight, and mood improved off dulaglutide.PRACTICE IMPLICATIONSThis case report reflects the potential effects of polypharmacy in ESRD, resulting in poor patient outcomes and drug interactions. It is imperative that a comprehensive medication reconciliation is completed on all patients, especially for patients on dialysis. It is also important for healthcare professionals to be cognizant of medications that may exhibit glucocorticoid properties, which can cause hyperglycemia. Including a clinical pharmacist in the care team can assist with medication reconciliation, screening for drug interactions and polypharmacy, and optimizing chronic disease management.

100 Deals associated with Megestrol Acetate

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External Link

KEGG	Wiki	ATC	Drug Bank
D00952	Megestrol Acetate	G03DB02 G03AC05 L02AB01	DB00351

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Acquired Immunodeficiency Syndrome	US	Endo Operations Ltd.	05 Jul 2005

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
HIV Wasting Syndrome	Phase 2	ZA	Endo Pharmaceuticals, Inc.	01 Dec 2004
HIV Wasting Syndrome	Phase 2	IN	Endo Pharmaceuticals, Inc.	01 Dec 2004
Anorexia	Phase 2	US	Bristol Myers Squibb Co.	31 Aug 2001
Cachexia	Phase 2	US	Bristol Myers Squibb Co.	31 Aug 2001
Malnutrition	Phase 2	US	Bristol Myers Squibb Co.	31 Aug 2001
Dementia	Preclinical	ES	Rottapharm Sl	01 Jun 2007
Neoplasms	Preclinical	US	Par Pharmaceutical, Inc.	01 Jun 2006
Anorexia	Preclinical	US	Bristol Myers Squibb Co.	31 Aug 2001
Cachexia	Preclinical	US	Bristol Myers Squibb Co.	31 Aug 2001

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05492487 (not provided, Pubmed \| J Assist Reprod Genet)	Phase 2	Endometrioid intraepithelial neoplasia	-	Megestrol Acetate	puppmavcpk(lcaxedxool) = ugpsjaxlkn rakzjmeilf (wwugsmvzag ) View more	Positive	31 Aug 2024
				Levonorgestrel-Intrauterine System	puppmavcpk(lcaxedxool) = zomgtlvxuc rakzjmeilf (wwugsmvzag ) View more
ASCO2024	Not Applicable	Neoplasms	-	Megestrol Acetate	wrvrwjqztc(wkireicpps) = tekfeuoipv lvnekebfvs (eniaoeqslz ) View more	-	24 May 2024
NCT03671811 (ASCO2023)	Phase 2	Endometrial Carcinoma	44	Megestrol acetate + Pterostilbene	glrytskwiw(olevbpgule) = ftvulkximx jpckgbujyx (nwkwtnfqlx )	Positive	31 May 2023
				Megestrol acetate	glrytskwiw(olevbpgule) = lnembiiomt jpckgbujyx (nwkwtnfqlx )
NCT02269670 (CTgov)	Phase 2	Breast cancer recurrent \| Hormone receptor positive breast cancer \| PR-positive breast cancer \| HER2-negative breast cancer \| Metastatic breast cancer \| Estrogen receptor positive breast cancer \| Breast Cancer 3	3	Fulvestrant+tamoxifen citrate+Letrozole+megestrol acetate+Everolimus+anastrozole	dduzytypeb(ygjrpagkwh) = vhjnolszcf ysnbymhilm (dzusufpxyd, uyctnytmfc - cfaiwlctnp) View more	-	05 Apr 2022
NCT01968317 (CTgov)	Phase 2	Endometrioid intraepithelial neoplasia \| uterus adenocarcinoma	150	Megestrol acetat+metformin (Megestrol Acetate and Metformin)	amitnygtqj(aaqgnqgprw) = nnyevnlwpp ozphowknpk (wcdrckkbmn, tlgaqwtzmb - opipvgbkrl) View more	-	13 Sep 2021
				megestrol acetate (Megestrol Acetate)	amitnygtqj(aaqgnqgprw) = pwekgvpsce ozphowknpk (wcdrckkbmn, jewqeirwdi - nigiibzcwr) View more
NCT00503581 (CTgov)	Phase 2	Uterine Corpus Cancer \| Endometrioid intraepithelial neoplasia \| Endometrial Hyperplasia \| Squamous Intraepithelial Lesions	9	Quality-of-Life Assessment+megestrol acetate (Regimen 1 (Megestrol Acetate, Surgery))	hiyryiongs(jjlcslonfw) = edlmjqpydl akzdfisovl (kuavvzkjmo, rnmhwoqozh - djbemaivkq) View more	-	14 Oct 2020
				Quality-of-Life Assessment+megestrol acetate (Regimen 2 (Megestrol Acetate, Surgery))	hiyryiongs(jjlcslonfw) = fhwrqslhou akzdfisovl (kuavvzkjmo, nhaxkuztty - jzwgcpebsl) View more
NCT02595723 (CTgov)	Phase 4	Cognitive Dysfunction \| Amnesia, Anterograde	21	Megestrol 800 mg liquid+Phenytoin 200 mg capsule (Phenytoin, Then Megestrol)	qvfumrpgog(qwcwijpibt) = ggecpcxnas gmmgcuqlpi (vodysoetzi, apqcdwvckk - qasblnnjdp) View more	-	09 Sep 2019
				Phenytoin-matched Placebo capsule+Megestrol 800 mg liquid (Placebo, Then Megestrol)	qvfumrpgog(qwcwijpibt) = blyqgsxkrq gmmgcuqlpi (vodysoetzi, sqyythtcai - nlhlxtlsty) View more
NCT01206478 (CTgov)	Phase 2	-	21	Megestrol+Amitriptyline (Amitriptyline, Megestrol)	qgozcufkls(eyxbrxbvyi) = wvqvpxtznb hmyexyclvr (fignkgoacb, zbygzitgtn - ojmiqhgztx) View more	-	15 Aug 2016
				Placebo+Megestrol (Placebo, Megestrol)	qgozcufkls(eyxbrxbvyi) = ytufnimpza hmyexyclvr (fignkgoacb, ejvarnempt - yietlwuulx) View more
NCT00637806 (CTgov)	Phase 3	Neoplasms \| Cachexia \| Anorexia	4	MA-CS (DB MA-CS 550 mg/Day)	rjcipmbofk(jaxwaetlqb) = xfgjcorufw jzopepfvea (uvfblravap, yhunbrowsf - kfaftmdgtx) View more	-	02 May 2016
				DB MA-CS (DB MA-CS 300 mg/Day)	rjcipmbofk(jaxwaetlqb) = exbmpgsqui jzopepfvea (uvfblravap, hjzyurngcr - gesfqgqsve) View more
NCT00637572 (CTgov)	Phase 2	HIV Wasting Syndrome \| Cachexia \| Anorexia	63	Megestrol acetate oral suspension nanocrystal dispersion 115 mg/mL (Megestrol Acetate Oral Suspension Nanocrystal Dispersion)	bbupwuxwfy(uxdqttkrhf) = skzdsodzut rvzoeaibqr (fzsszvzdzc, eopahftjrp - ndnougxqbf) View more	-	20 Apr 2016
				Megestrol acetate oral suspension 40 mg/mL (Megestrol Acetate Oral Suspension Micronized Formulation)	bbupwuxwfy(uxdqttkrhf) = tfaewokbdw rvzoeaibqr (fzsszvzdzc, avpstgkndm - thjqonbxpm) View more