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- H3B-6545 / Eisai
H3B-6545 in women with locally advanced/metastatic estrogen receptor-positive (ER+), HER2 negative ( (Hall D1) - Apr 24, 2024 - Abstract #ASCO2024ASCO_2574;
P1/2
H3B-6545 had a low rate of G ?3 TEAEs and showed clinically meaningful antitumor activity in heavily pretreated female patients with ER+, HER2
- Ibrance (palbociclib) / Pfizer, H3B-6545 / Eisai
H3B-6545 + palbociclib in patients (pts) with locally advanced/metastatic estrogen receptor-positive (ER+), HER2 negative ( (Hall A; Poster Bd #: 29) - Apr 24, 2024 - Abstract #ASCO2024ASCO_2481;
P1
H3B-6545 300 mg + palbo (100/125 mg) had manageable safety and encouraging preliminary antitumor activity. Further studies are warranted to identify the RP2D.
- | H3B-6545 / Eisai
Trial completion date, Combination therapy, Metastases: H3B-6545-G000-102: A Study of H3B-6545 in Combination With Palbociclib in Women With Advanced or Metastatic Estrogen Receptor-Positive Human Epidermal Growth Factor Receptor-2 (HER2)-Negative Breast Cancer (clinicaltrials.gov) - Mar 27, 2024
P1, N=31, Active, not recruiting, Sponsor: Eisai Inc.
Further studies are warranted to identify the RP2D. Trial completion date: Mar 2024 --> Aug 2024
- H3B-6545 / Eisai
Phase classification, Combination therapy, Metastases: H3B-6545-G000-102: A Study of H3B-6545 in Combination With Palbociclib in Women With Advanced or Metastatic Estrogen Receptor-Positive Human Epidermal Growth Factor Receptor-2 (HER2)-Negative Breast Cancer (clinicaltrials.gov) - Mar 22, 2024
P1, N=31, Active, not recruiting, Sponsor: Eisai Inc.
Trial completion date: Mar 2024 --> Aug 2024 Phase classification: P1b --> P1
- |||| H3B-6545 / Eisai
Trial completion, Metastases: H3B-6545-A001-101: Trial of H3B-6545, in Women With Locally Advanced or Metastatic Estrogen Receptor-positive, HER2 Negative Breast Cancer (clinicaltrials.gov) - Dec 26, 2023
P1/2, N=206, Completed, Sponsor: Eisai Inc.
Phase classification: P1b --> P1 Active, not recruiting --> Completed
- H3B-6545 / Eisai
Phase I study of H3B-6545 in patients (pts) with estrogen receptor-positive (ER+) breast cancer (Hall 401) - Oct 6, 2023 - Abstract #ESMOAsia2023ESMO_Asia_418;
P1
Among 6 pts with ESR1 Y537S, CBR was 83% with 1 PR. Conclusions H3B-6545 450 mg QD had a manageable safety profile and showed preliminary antitumor effect in pts with heavily pretreated, ER+, HER2-negative mBC.
- | H3B-6545 / Eisai
Trial completion date, Trial primary completion date: Study of H3B-6545 in Japanese Women With Estrogen Receptor (ER)-Positive, Human Epidermal Growth Factor Receptor 2 (HER2)-Negative Breast Cancer (clinicaltrials.gov) - Sep 26, 2023
P1, N=33, Active, not recruiting, Sponsor: Eisai Co., Ltd.
Conclusions H3B-6545 450 mg QD had a manageable safety profile and showed preliminary antitumor effect in pts with heavily pretreated, ER+, HER2-negative mBC. Trial completion date: Nov 2023 --> Aug 2024 | Trial primary completion date: Nov 2023 --> Aug 2024
- ||| H3B-6545 / Eisai
Enrollment change, Metastases: H3B-6545-A001-101: Trial of H3B-6545, in Women With Locally Advanced or Metastatic Estrogen Receptor-positive, HER2 Negative Breast Cancer (clinicaltrials.gov) - Mar 23, 2023
P1/2, N=206, Active, not recruiting, Sponsor: Eisai Inc.
Trial completion date: Nov 2023 --> Aug 2024 | Trial primary completion date: Nov 2023 --> Aug 2024 N=151 --> 206
- || H3B-6545 / Eisai
Trial completion date, Trial primary completion date, Metastases: H3B-6545-A001-101: Trial of H3B-6545, in Women With Locally Advanced or Metastatic Estrogen Receptor-positive, HER2 Negative Breast Cancer (clinicaltrials.gov) - Feb 2, 2023
P1/2, N=151, Active, not recruiting, Sponsor: Eisai Inc.
N=151 --> 206 Trial completion date: Dec 2022 --> Oct 2023 | Trial primary completion date: Dec 2022 --> Oct 2023
- | H3B-6545 / Eisai
Trial completion date, Trial primary completion date: Study of H3B-6545 in Japanese Women With Estrogen Receptor (ER)-Positive, Human Epidermal Growth Factor Receptor 2 (HER2)-Negative Breast Cancer (clinicaltrials.gov) - Dec 20, 2022
P1, N=33, Active, not recruiting, Sponsor: Eisai Co., Ltd.
Trial completion date: Dec 2022 --> Oct 2023 | Trial primary completion date: Dec 2022 --> Oct 2023 Trial completion date: Feb 2023 --> Nov 2023 | Trial primary completion date: Feb 2023 --> Nov 2023
- || H3B-6545 / Eisai
Enrollment closed: Study of H3B-6545 in Japanese Women With Estrogen Receptor (ER)-Positive, Human Epidermal Growth Factor Receptor 2 (HER2)-Negative Breast Cancer (clinicaltrials.gov) - Nov 28, 2022
P1, N=33, Active, not recruiting, Sponsor: Eisai Co., Ltd.
Trial completion date: Feb 2023 --> Nov 2023 | Trial primary completion date: Feb 2023 --> Nov 2023 Recruiting --> Active, not recruiting
- || H3B-6545 / Eisai
Trial completion date, Trial primary completion date, Metastases: H3B-6545-A001-101: Trial of H3B-6545, in Women With Locally Advanced or Metastatic Estrogen Receptor-positive, HER2 Negative Breast Cancer (clinicaltrials.gov) - Jun 7, 2022
P1/2, N=170, Active, not recruiting, Sponsor: H3 Biomedicine Inc.
Recruiting --> Active, not recruiting Trial completion date: Jun 2023 --> Dec 2022 | Trial primary completion date: Jun 2023 --> Dec 2022
- | H3B-6545 / Eisai
Preclinical, Journal: Covalent ERα Antagonist H3B-6545 Demonstrates Encouraging Preclinical Activity in Therapy-Resistant Breast Cancer. (Pubmed Central) - Jun 4, 2022
P1, P1/2,
In summary, the compelling preclinical activity of H3B-6545 supports its further development for the potential treatment of endocrine therapy-resistant ERα+ breast cancer harboring wild-type or mutant ESR1, as demonstrated by the ongoing clinical trials (NCT03250676, NCT04568902, NCT04288089). H3B-6545 is an ERα covalent antagonist that exhibits encouraging preclinical activity against CDK4/6i naïve and resistant ERαWT and ERαMUT tumors.
- || H3B-6545 / Eisai
Enrollment closed, Metastases: H3B-6545-A001-101: Trial of H3B-6545, in Women With Locally Advanced or Metastatic Estrogen Receptor-positive, HER2 Negative Breast Cancer (clinicaltrials.gov) - May 31, 2022
P1/2, N=170, Active, not recruiting, Sponsor: H3 Biomedicine Inc.
H3B-6545 is an ERα covalent antagonist that exhibits encouraging preclinical activity against CDK4/6i naïve and resistant ERαWT and ERαMUT tumors. Recruiting --> Active, not recruiting
- || H3B-6545 / Eisai
Enrollment closed, Combination therapy, Metastases: H3B-6545-G000-102: A Study of H3B-6545 in Combination With Palbociclib in Women With Advanced or Metastatic Estrogen Receptor-Positive Human Epidermal Growth Factor Receptor-2 (HER2)-Negative Breast Cancer (clinicaltrials.gov) - May 31, 2022
P1b, N=36, Active, not recruiting, Sponsor: H3 Biomedicine Inc.
Recruiting --> Active, not recruiting Recruiting --> Active, not recruiting
- || H3B-6545 / Eisai
Trial completion date, Trial primary completion date, Metastases: H3B-6545-A001-101: Trial of H3B-6545, in Women With Locally Advanced or Metastatic Estrogen Receptor-positive, HER2 Negative Breast Cancer (clinicaltrials.gov) - Apr 12, 2022
P1/2, N=170, Recruiting, Sponsor: H3 Biomedicine Inc.
Recruiting --> Active, not recruiting Trial completion date: Sep 2022 --> Jun 2023 | Trial primary completion date: Mar 2022 --> Jun 2023
- || H3B-6545 / Eisai
Enrollment change: Study of H3B-6545 in Japanese Women With Estrogen Receptor (ER)-Positive, Human Epidermal Growth Factor Receptor 2 (HER2)-Negative Breast Cancer (clinicaltrials.gov) - Jan 25, 2022
P1, N=33, Recruiting, Sponsor: Eisai Co., Ltd.
Trial completion date: Sep 2022 --> Jun 2023 | Trial primary completion date: Mar 2022 --> Jun 2023 N=18 --> 33
- || H3B-6545 / Eisai
Trial completion date, Trial primary completion date, Metastases: H3B-6545-A001-101: Trial of H3B-6545, in Women With Locally Advanced or Metastatic Estrogen Receptor-positive, HER2 Negative Breast Cancer (clinicaltrials.gov) - Nov 4, 2021
P1/2, N=170, Recruiting, Sponsor: H3 Biomedicine Inc.
N=18 --> 33 Trial completion date: May 2025 --> Sep 2022 | Trial primary completion date: Nov 2024 --> Mar 2022
- || H3B-6545 / Eisai
Trial completion date, Trial primary completion date, Metastases: H3B-6545-A001-101: Trial of H3B-6545, in Women With Locally Advanced or Metastatic Estrogen Receptor-positive, HER2 Negative Breast Cancer (clinicaltrials.gov) - Nov 1, 2021
P1/2, N=170, Recruiting, Sponsor: H3 Biomedicine Inc.
Trial completion date: May 2025 --> Sep 2022 | Trial primary completion date: Nov 2024 --> Mar 2022 Trial completion date: Jan 2024 --> May 2025 | Trial primary completion date: Jan 2022 --> Nov 2024
- H3B-6545 / Eisai
H3B-6545, a novel selective estrogen receptor covalent antagonist (SERCA), in estrogen receptor positive (ER+), human epidermal growth factor receptor 2 negative (HER2-) advanced breast cancer - A phase II study (Hall 1) - Oct 26, 2021 - Abstract #SABCS2021SABCS_558;
Clinical activity was consistent across the various subgroups. Tumors harboring the constitutionally active ESR1 Y537S mutation may present higher ERα activity, and consequently enrich for luminal A traits and demonstrate greater lineage dependence on ERα.
- Ibrance (palbociclib) / Pfizer, H3B-6545 / Eisai
H3B-6545 in combination with palbociclib in women with metastatic estrogen receptor-positive (ER+), human epidermal growth factor receptor 2 (HER2)-negative breast cancer, phase 1b study (Hall 1) - Oct 26, 2021 - Abstract #SABCS2021SABCS_551;
P1b
The combination of H3B-6545 (up to 300 mg dose) and palbociclib (up to 125 mg dose) was well-tolerated and demonstrated preliminary anti-tumor activity in heavily pretreated pts with ER+, HER2- mBC. ClinicalTrials.gov Identifier : NCT04288089.
- | H3B-6545 / Eisai
Trial completion date, Trial primary completion date: Study of H3B-6545 in Japanese Women With Estrogen Receptor (ER)-Positive, Human Epidermal Growth Factor Receptor 2 (HER2)-Negative Breast Cancer (clinicaltrials.gov) - Oct 22, 2021
P1, N=18, Recruiting, Sponsor: Eisai Co., Ltd.
ClinicalTrials.gov Identifier : NCT04288089. Trial completion date: Apr 2022 --> Feb 2023 | Trial primary completion date: Apr 2022 --> Feb 2023
- | H3B-6545 / Eisai
Trial completion date, Trial primary completion date: Study of H3B-6545 in Japanese Women With Estrogen Receptor (ER)-Positive, Human Epidermal Growth Factor Receptor 2 (HER2)-Negative Breast Cancer (clinicaltrials.gov) - Oct 14, 2021
P1, N=18, Recruiting, Sponsor: Eisai Co., Ltd.
Trial completion date: Apr 2022 --> Feb 2023 | Trial primary completion date: Apr 2022 --> Feb 2023 Trial completion date: Jan 2022 --> Apr 2022 | Trial primary completion date: Jan 2022 --> Apr 2022
- |||| H3B-6545 / Eisai
H3B-6545 is high on my list for a future trial if (when) my new ET/CDK 4/6 inhibitor fails me. Was super excited to see Dr. @ErikaHamilton9’s poster at #ASCO21 and here this report. #bcsm #metastaticbreastcancer (Twitter) - Jun 29, 2021
- ||||| H3B-6545 / Eisai
Dr. @ErikaHamilton9 discusses the results of a Phase I/II study (NCT03250676) of H3B-6545 for the treatment of estrogen receptor (ER)-positive, HER2-negative advanced breast cancer refractory to endocrine therapy. https://t.co/VUEVXpsPvy (Twitter) - Jun 29, 2021
P1/2
- ||||| Venclexta (venetoclax) / Roche, AbbVie, H3B-6545 / Eisai, LY3484356 / Eli Lilly
Clinical, IO biomarker: HR+ Metastatic Breast Cancer, #ASCO21 update • Venetoclax + Fluvestrant, a BCL-2 inhibitor, VERONICA, negative study, 1004 • ER-alpha inhibitor H3B-6545, 1018, promising, in ESR mutant HR+ MBC • New SERD, Giresdestrant, SAR4399859, LY3484356, possible clinical activities (Twitter) - Jun 6, 2021
- ||| H3B-6545 / Eisai
The #OncoAlertTopTweet 🚨for DAY2⃣of #ASCO21 @ErikaHamilton9 👩⚕️🇺🇸of @SarahCannonDocs presenting abstract 1018 Study of H3B-6545(SERCA) in ER+ HER2- advanced #BreastCancer #bcsm Thanks, @weoncologists (Twitter) - Jun 6, 2021
- |||| H3B-6545 / Eisai
P1/2 data: H3B-6545 is an oral medication (yay!) that inactivates ERalpha, including those receptors that have mutated to get around other endocrine therapies. Dr @ErikaHamilton9 has 2 posters on H3B-6545, describing a phase 1 and a phase 1/2 trial (abstracts 1059 and 1018) #ASCO21 #bcsm (Twitter) - Jun 5, 2021
- |||| H3B-6545 / Eisai
Clinical, Adverse events, Lymphopenia: H3B-6545, ER-alpha covalent inhibitor shows clinical activity in the ESR1 mutated HR+ MBC. It has a unique side effect bradycardia and lymphopenia but well tolerated. Looking forward to seeing the randomized study outcome in the future. #bcsm #ASCO21 https://t.co/3Lay4B9oV3 (Twitter) - Jun 4, 2021
- Ibrance (palbociclib) / Pfizer, H3B-6545 / Eisai
[VIRTUAL] Phase 1b study of H3B-6545 in combination with palbociclib in women with metastatic estrogen receptor–positive (ER+), human epidermal growth factor receptor 2 (HER2)-negative breast cancer. () - Apr 29, 2021 - Abstract #ASCO2021ASCO_3717;
P1b
Trial completion date: Jan 2022 --> Apr 2022 | Trial primary completion date: Jan 2022 --> Apr 2022 H3B-6545, in combination with palbociclib, was well-tolerated.
- H3B-6545 / Eisai
[VIRTUAL] Relative bioavailability of H3B-6545 tablets versus capsules and drug-drug interaction between H3B-6545 and pantoprazole. () - Apr 29, 2021 - Abstract #ASCO2021ASCO_3714;
Plasma PK of H3B-6545 is similar between tablets and capsules, and in the absence or presence of pantoprazole . Concurrent use of gastric acid reducers had a minimal effect on H3B-6545 exposure and was not considered clinically meaningful.
- H3B-6545 / Eisai
[VIRTUAL] Phase I/II study of H3B-6545, a novel selective estrogen receptor covalent antagonist (SERCA), in estrogen receptor positive (ER+), human epidermal growth factor receptor 2 negative (HER2-) advanced breast cancer. () - Apr 28, 2021 - Abstract #ASCO2021ASCO_1311;
P1/2
H3B-6545 has a manageable safety profile and demonstrated single-agent anti-tumor activity in heavily pretreated ER+, HER2- mBC patients . Clinical activity was observed in pts with ESR1 mutations.
- ||| H3B-6545 / Eisai
H3B-6545はESR1 Y537S変異やCDK4/6阻害薬・フルベストラントを含む治療歴の多いER＋HER2－転移乳癌に対し有望【SABCS2020】：がんナビ サンアントニオ乳がんシンポジウムからのニュースです。今後の開発に期待します。 #乳がん #SABCS20 https://t.co/2VkXfo0c3i (Twitter) - Dec 11, 2020
- ||||| H3B-6545 / Eisai
P1/2 data: Join @ErikaHamilton9 this afternoon's #SABCS20 poster discussion on phase I/II trial of H3B-6545, a novel selective estrogen receptor covalent antagonist (SERCA), in ER+, human epidermal growth factor receptor 2 negative (HER2-) advanced breast cancer, today at 2:15pm CT. (Twitter) - Dec 10, 2020
- || H3B-6545 / Eisai
Enrollment open: Study of H3B-6545 in Japanese Women With Estrogen Receptor (ER)-Positive, Human Epidermal Growth Factor Receptor 2 (HER2)-Negative Breast Cancer (clinicaltrials.gov) - Nov 18, 2020
P1, N=18, Recruiting, Sponsor: Eisai Co., Ltd.
Clinical activity was observed in pts with ESR1 mutations. Not yet recruiting --> Recruiting
- H3B-6545 / Eisai
[VIRTUAL] Phase I/II trial of H3B-6545, a novel selective estrogen receptor covalent antagonist (SERCA), in estrogen receptor positive (ER+), human epidermal growth factor receptor 2 negative (HER2-) advanced breast cancer (Channel 2) - Oct 2, 2020 - Abstract #SABCS2020SABCS_1237;
Median PFS, in all pts and in pts with clonal ESR1 Y537S was 3.7 months and 7.3 months, respectively. Conclusions : H3B-6545 has a manageable safety profile and demonstrated single-agent anti-tumor activity in heavily pretreated ER+, HER2- mBC patients including those with a constitutively active clonal ESR1 Y537S mutation.
- H3B-6545 / Eisai
[VIRTUAL] Development of H3B-6545, a first-in-class oral selective ER covalent antagonist (SERCA), for the treatment of ERaWT and ERaMUT breast cancer (OnDemand) - Oct 2, 2020 - Abstract #SABCS2020SABCS_800;
P1/2
H3B-6545 as a monotherapy demonstrates superior anti-tumor activity relative to fulvestrant across a set of CDK4/6 inhibitor naïve ERα WT and ERα Y537S cell line-derived xenograft (CDX)/patient-derived xenograft (PDX) models, with regressions being noted in both the ERα WT and ERα MUT settings...Lastly, improved activity and duration of response are noted when H3B-6545 is combined with several targeted therapies, including CDK4/6 inhibitors palbociclib and abemaciclib across a range of ERα WT and ERα Y537S CDX/PDX models...Consistent with the preclinical data, H3B-6545 demonstrated promising clinical activity among these pts with clonal Y537S mutations, with a median progression free survival of 7.3 months and an overall response rate of 25% (3 confirmed partial responses). In summary, these compelling preclinical data coupled with emerging clinical activity in heavily pretreated poor prognosis pts support further development of H3B-6545 as monotherapy or combination treatment.
- H3B-6545 / Eisai
[VIRTUAL] Pharmacokinetics of H3B-6545 in patients with locally advanced or metastatic estrogen receptor-positive HER2 negative breast cancer (ER+ and HER2- BC) (OnDemand) - Oct 2, 2020 - Abstract #SABCS2020SABCS_792;
P1/2
H3B-6545 PK profiles in breast cancer patients were well described by a one-compartment disposition model with no significant effect of demographics, liver and renal function. When administered with a high fat meal, H3B-6545 exposure was modestly increased.
- || H3B-6545 / Eisai
New P1 trial: Study of H3B-6545 in Japanese Women With Estrogen Receptor (ER)-Positive, Human Epidermal Growth Factor Receptor 2 (HER2)-Negative Breast Cancer (clinicaltrials.gov) - Sep 28, 2020
P1, N=18, Not yet recruiting, Sponsor: Eisai Co., Ltd.
- ||| H3B-6545 / Eisai
Enrollment open, Trial completion date, Trial primary completion date, Metastases: H3B-6545-A001-101: Trial of H3B-6545, in Women With Locally Advanced or Metastatic Estrogen Receptor-positive, HER2 Negative Breast Cancer (clinicaltrials.gov) - Sep 9, 2020
P1/2, N=148, Recruiting, Sponsor: H3 Biomedicine Inc.
When administered with a high fat meal, H3B-6545 exposure was modestly increased. Active, not recruiting --> Recruiting | Trial completion date: Jan 2022 --> Jan 2024 | Trial primary completion date: Jul 2020 --> Jan 2022
- || H3B-6545 / Eisai
Enrollment open, Combination therapy, Metastases: H3B-6545-G000-102: A Study of H3B-6545 in Combination With Palbociclib in Women With Advanced or Metastatic Estrogen Receptor-Positive Human Epidermal Growth Factor Receptor-2 (HER2)-Negative Breast Cancer (clinicaltrials.gov) - Jul 21, 2020
P1b, N=36, Recruiting, Sponsor: H3 Biomedicine Inc.
Active, not recruiting --> Recruiting | Trial completion date: Jan 2022 --> Jan 2024 | Trial primary completion date: Jul 2020 --> Jan 2022 Not yet recruiting --> Recruiting
- || H3B-6545 / Eisai
New P1 trial, Combination therapy, Metastases: H3B-6545-G000-102: A Study of H3B-6545 in Combination With Palbociclib in Women With Advanced or Metastatic Estrogen Receptor-Positive Human Epidermal Growth Factor Receptor-2 (HER2)-Negative Breast Cancer (clinicaltrials.gov) - Feb 27, 2020
P1b, N=36, Not yet recruiting, Sponsor: H3 Biomedicine Inc.
- | H3B-6545 / Eisai
Preclinical, Journal: Characterization of the metabolites of H3B-6545 in vitro and in vivo by using ultra-high performance liquid chromatography combined with electrospray ionization linear ion trap-orbitrap tandem mass spectrometry. (Pubmed Central) - Feb 26, 2020
Among these metabolites, M1, M5, M7 and M10 were newly found and reported for the first time. The metabolic pathways of H3B-6545 included deamination (M8 and M9), dealkylation (M2, M3 and M10), N-hydroxylation (M6), hydroxylation (M1 and M4), formation of amide derivatives (M5 and M7) and GSH conjugation (G1).
- | H3B-6545 / Eisai
Preclinical, Journal: H3B-6545, a selective estrogen receptor covalent antagonist, prevents bone loss in ovariectomized Sprague-Dawley rats. (Pubmed Central) - Jan 24, 2020
The metabolic pathways of H3B-6545 included deamination (M8 and M9), dealkylation (M2, M3 and M10), N-hydroxylation (M6), hydroxylation (M1 and M4), formation of amide derivatives (M5 and M7) and GSH conjugation (G1). No abstract available
- || H3B-6545 / Eisai
Enrollment closed, Trial completion date, Trial primary completion date, Metastases: H3B-6545-A001-101: Trial of H3B-6545, in Women With Locally Advanced or Metastatic Estrogen Receptor-positive, HER2 Negative Breast Cancer (clinicaltrials.gov) - Jan 18, 2020
P1/2, N=127, Active, not recruiting, Sponsor: H3 Biomedicine Inc.
No abstract available Recruiting --> Active, not recruiting | Trial completion date: May 2020 --> Jan 2022 | Trial primary completion date: Nov 2019 --> Jul 2020
- || H3B-6545 / Eisai
PK/PD data, Journal: Pharmacokinetics and metabolism of H3B-6545, a selective estrogen receptor covalent antagonist, in dog plasma by liquid chromatography combined with electrospray ionization tandem mass spectrometry. (Pubmed Central) - Dec 20, 2019
Additionally, the metabolites present in dog plasma were identified by LC-ESI-Q-Exactive-Orbitrap-MS and their identities were characterized by retention times, accurate masses and fragment ions. The metabolic pathways referred to N-demethylation, N-dealkylation, deamination, aldehyde oxidation, aldehyde reduction and formation of amide.
- || H3B-6545 / Eisai
PK/PD data, Preclinical, Journal: Nonclinical pharmacokinetics and in vitro metabolism of H3B-6545, a novel selective ERα covalent antagonist (SERCA). (Pubmed Central) - Nov 14, 2019
The metabolic pathways referred to N-demethylation, N-dealkylation, deamination, aldehyde oxidation, aldehyde reduction and formation of amide. We report on the absorption and metabolic fate and disposition of H3B-6545 in rats and dogs and illustrate that in vitro-in vivo correlation of clearance is possible for targeted covalent inhibitors, provided reactivity is not a predominant mechanism of clearance.
- || H3B-6545 / Eisai
Trial completion date, Trial primary completion date, Metastases: H3B-6545-A001-101: Trial of H3B-6545, in Women With Locally Advanced or Metastatic Estrogen Receptor-positive, HER2 Negative Breast Cancer (clinicaltrials.gov) - May 30, 2019
P1/2, N=110, Recruiting, Sponsor: H3 Biomedicine Inc.
We report on the absorption and metabolic fate and disposition of H3B-6545 in rats and dogs and illustrate that in vitro-in vivo correlation of clearance is possible for targeted covalent inhibitors, provided reactivity is not a predominant mechanism of clearance. Trial completion date: Dec 2019 --> May 2020 | Trial primary completion date: Apr 2019 --> Nov 2019
- | H3B-6545 / Eisai
Trial completion date, Trial primary completion date, Metastases: H3B-6545-A001-101: Trial of H3B-6545, in Women With Locally Advanced or Metastatic Estrogen Receptor-positive, HER2 Negative Breast Cancer (clinicaltrials.gov) - Jul 30, 2018
P1/2, N=110, Recruiting, Sponsor: H3 Biomedicine Inc.
Trial completion date: Dec 2019 --> May 2020 | Trial primary completion date: Apr 2019 --> Nov 2019 Trial completion date: Apr 2019 --> Dec 2019 | Trial primary completion date: Dec 2018 --> Apr 2019
- |||| H3B-6545 / Eisai
Enrollment open, Metastases: H3B-6545-A001-101: Trial of H3B-6545, in Women With Locally Advanced or Metastatic Estrogen Receptor-positive, HER2 Negative Breast Cancer (clinicaltrials.gov) - Aug 29, 2017
P1/2, N=110, Recruiting, Sponsor: H3 Biomedicine Inc.
Trial completion date: Apr 2019 --> Dec 2019 | Trial primary completion date: Dec 2018 --> Apr 2019 Not yet recruiting --> Recruiting