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Last update 08 May 2025

HTR3A x NK1R

Last update 08 May 2025

Basic Info

Related Targets

HTR3ANK1R

Drugs associated with HTR3A x NK1R

HR-20013

Target

HTR3A x NK1R

Mechanism

5-HT3A receptor antagonists [+1]

Active Org.

Fujian Suncadia Pharmaceuticals Co Ltd.

Originator Org.

Fujian Suncadia Pharmaceuticals Co Ltd.

Active Indication

Chemotherapy-induced nausea and vomiting [+4]

Inactive Indication-

Drug Highest PhaseNDA/BLA

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with HTR3A x NK1R

CTR20243064

/ RecruitingPhase 3

以盐酸帕洛诺司琼为对照，评价注射用HR20013用于预防中致吐风险抗肿瘤药物引起恶心呕吐的有效性和安全性研究—多中心、随机、双盲双模拟、阳性对照Ⅲ期临床研究

[Translation] A multicenter, randomized, double-blind, double-dummy, positive-controlled phase III clinical study to evaluate the efficacy and safety of HR20013 for injection in preventing nausea and vomiting caused by anticancer drugs with moderate emetogenic risk, using palonosetron hydrochloride as a control

评价注射用HR20013用于预防中致吐风险抗肿瘤药物引起恶心呕吐的有效性；评价注射用HR20013用于预防中致吐风险抗肿瘤药物引起恶心呕吐的安全性和HR20013的群体药代动力学特征

[Translation]

To evaluate the effectiveness of HR20013 for injection in preventing nausea and vomiting caused by anticancer drugs with moderate emetogenic risk; to evaluate the safety of HR20013 for injection in preventing nausea and vomiting caused by anticancer drugs with moderate emetogenic risk and the population pharmacokinetic characteristics of HR20013

Start Date03 Sep 2024

Sponsor / Collaborator

Fujian Suncadia Pharmaceuticals Co Ltd.

NCT06554184

/ RecruitingPhase 3

A Randomized Phase III Study Evaluating the Efficacy and Safety of HR20013 for Nausea and Vomiting Associated With Moderate Emetic Risk Anticancer Agents

This study is aimed to evaluate the efficacy and safety of HR20013 versus palonosetron for nausea and vomiting associated with moderate emetic risk anticancer agents

Start Date03 Sep 2024

Sponsor / Collaborator

Fujian Suncadia Pharmaceuticals Co Ltd.

100 Clinical Results associated with HTR3A x NK1R

100 Translational Medicine associated with HTR3A x NK1R

0 Patents (Medical) associated with HTR3A x NK1R

Literatures (Medical) associated with HTR3A x NK1R

01 Apr 2025·JCO Precision Oncology

Personalized Prophylactic Antiemetic Regimens for Control of Chemotherapy-Induced Nausea and Vomiting by Pharmacogenetic Analysis of Three Receptor Genes: HTR3A , HTR3B , TACR1

Article

Author: Yeo, Horatio L. ; Ou, Menglin ; Li, Leung V. ; Ma, Suk-Ling ; Lai, Kwai T. ; Tang, Nelson L.S. ; Yeo, Winnie ; Ko, Wan-Hei ; Mo, Frankie K.F. ; Huang, JingHan ; Lau, Thomas K.H. ; Pang, Elizabeth

PURPOSEContemporary prophylactic antiemetic regimens have improved the control of chemotherapy-induced nausea and vomiting (CINV). However, over 50% of patients still suffer from nausea. This study aimed to correlate the genetic determinants of individual patients with the efficacy of three prophylactic antiemetic regimens.METHODS Patients with breast cancer in two previously reported prospective antiemetic studies consented for the present pharmacogenetic study. Before high-emetogenic doxorubicin and cyclophosphamide (AC) (neo)adjuvant chemotherapy, they received a combination of antiemetic prophylaxis: regimen A and regimen B were, respectively, aprepitant/ondansetron/dexamethasone with or without olanzapine; regimen C was netupitant/palonosetron/dexamethasone. The effectiveness of antiemetic regimens was mainly assessed by complete protection (CP) rates. Patients' genotypes in three genes, HTR3A , HTR3B and TACR1 , were analyzed. RESULTS Patients who were homozygous TT (p.129Tyr) of a non-nonsynonymous variant in HTR3B rs1176744 and homozygous GG of TACR1 rs3821313 had better outcome with regimen B. Digenic interaction analysis further reveals interaction between rs1176744 and rs3821313. Homozygotes TT of rs1176744 and homozygotes GG of rs3821313 achieved the highest CP rate with regimen B (10/12 patients; 83%), in contrast to only 29% (7/24) with regimen A ( P = .0027). Homozygotes GG in both HTR3A rs1176722 and TACR1 rs3821313 showed the poorest response to regimen A with a CP rate of 17% (2/12), whereas patients given regimen B had the highest CP rate (70%; 7/10; P = .0159). The findings were confirmed upon logistic regression adjusted for clinical factors. CONCLUSIONThe present study confirmed our hypothesis that among Chinese patients with breast cancer who received AC, the selection of optimal antiemetic prophylaxis may be aided by assessing an individual's pharmacogenetic profile. It also highlights a novel digenic interaction that has not been known before for pharmacogenetic analysis.

01 Apr 2025·Supportive Care in Cancer

Efficacy of triplet antiemetic prophylaxis against chemotherapy-induced nausea and vomiting in patients with soft tissue sarcomas receiving consecutive-day doxorubicin and ifosfamide therapy

Article

Author: Hoshino, Ryo ; Fujii, Hironori ; Tsugita, Masanori ; Nagano, Akihito ; Yamada, Yunami ; Akiyama, Haruhiko ; Iihara, Hirotoshi ; Suzuki, Akio ; Kobayashi, Ryo ; Hara, Koki

BACKGROUNDDoxorubicin and ifosfamide (AI) therapy for soft tissue sarcomas (STS) is given as a 5-day continuous-dose chemotherapy regimen, and classified as carrying high emetic risk. The purpose of this study was to evaluate the efficacy of triplet antiemetic prophylaxis, consisting of a 5-HT₃ receptor antagonist, dexamethasone (DEX), and an NK₁ receptor antagonist, against chemotherapy-induced nausea and vomiting (CINV) induced by AI therapy, and to determine the prophylactic antiemetic effect of the addition of olanzapine (OLZ) to this triplet antiemetic prophylaxis in cases of poor antiemesis.PATIENTS AND METHODSPatients who received AI therapy for STS between October 2011 and October 2022 were included in this retrospective study. Patients who did not receive the standard triplet antiemetic prophylaxis of granisetron, DEX, and aprepitant were excluded. Primary endpoint was the rate of complete response (CR) and secondary endpoint was the rate of significant nausea prevention during the acute (days 1-6), delayed (days 7-10), and overall (days 1-10) periods. In addition, CR rate and significant nausea prevention during the acute phase were compared before and after the addition of OLZ in patients who received OLZ as antiemetic prophylaxis in the subsequent cycle due to poor antiemetic control.RESULTSA total of 58 patients were analyzed. CR rate for all patients was 32.8% in the acute phase, 53.4% in the delayed phase, and 29.3% in the overall period. The significant nausea prevention rate was 19.0%, 43.1%, and 13.8%, respectively. Sixteen patients received additional OLZ as an antiemetic prophylaxis. Their CR rate before and after the addition of OLZ during the acute phase improved significantly, from 6.3 to 43.8% (P = 0.041). The rate of significant nausea prevention tended to improve, from 6.3 to 43.8% (P = 0.077).CONCLUSIONControl of CINV with granisetron, DEX, and aprepitant was poor in patients with STS receiving AI therapy. Addition of OLZ to this standard triplet antiemetic prophylaxis may improve CINV control in the subsequent cycle in patients who experience inadequate CINV control during their first cycle of AI therapy.

01 Mar 2025·Supportive Care in Cancer

MASCC antiemetic consensus recommendations: resource-limited settings

Article

Author: Smit, Teresa ; Ostwal, Vikas ; Bosnjak, Snezana M ; Aapro, Matti ; Zilic, Ana ; Iihara, Hirotoshi ; Gralla, Richard ; Radhakrishnan, Venkatraman

PURPOSEPrevention of chemotherapy-induced nausea and vomiting (CINV) remains an essential supportive care need for patients receiving cancer treatment. Due to inadequate access to antiemetics in many countries, guideline-recommended CINV prophylaxis is not always possible. Our goal was to formulate antiemetic recommendations for resource-limited settings and define alternative antiemetic regimens for the CINV prophylaxis after highly (HEC) and moderately emetic chemotherapy (MEC), when NK₁-receptor antagonists are not accessible.METHODSThe recommendations based on the MASCC/ESMO 2023 Guideline Update were considered as the best option. The stratification based on a meta-analysis published by Filetti et al. (2023) was used in order to select and rank NK₁-receptor antagonist-free regimens by their probability of achieving complete response. Alternative NK₁-receptor antagonist-free regimens based on olanzapine are proposed, ranked by their efficacy as "better" and "good" options when "best" regimens recommended by the MASCC/ESMO 2023 Guideline Update were not available or affordable.RESULTSFor the prevention of acute CINV, in patients receiving HEC (HEC-cisplatin and AC-HEC) with no access to an NK₁-receptor antagonist, a 3-drug regimen including single doses of a 5-HT₃-receptor antagonist, dexamethasone, and olanzapine given before chemotherapy is recommended as an alternative option. Olanzapine and dexamethasone are recommended days 2-4 after chemotherapy. The O10PD regimen (10 mg olanzapine, palonosetron, and dexamethasone) is suggested as the alternative regimen in the category "better." Other 5-HT₃-receptor antagonists (ondansetron, granisetron) may be used if palonosetron is not affordable (category "good"). No guideline is possible for the alternative regimens to prevent acute CINV following MEC because of limited (carboplatin, AUC ≥ 5) or unavailable data (oxaliplatin chemotherapy in women aged < 50 years). Limited data are also available on the management of CINV following trastuzumab-deruxtecan.CONCLUSIONThe most effective prevention of CINV recommended by the MASCC/ESMO 2023 Guideline Update must be given when available and affordable. These recommendations were developed to facilitate decision on which regimen to use when the best MASCC/ESMO 2023 recommended regimen is not accessible because NK₁-receptor antagonists are either not available or not affordable.

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