TAK-243 (MLN7243) Clinical Trials

Size	Price	Qty
2mg	USD 147
5mg	USD 197

Clinical Trials

Multiple Phase I clinical trials have evaluated TAK-243 in advanced solid tumors and various hematologic malignancies, including relapsed or refractory acute myeloid leukemia, myelodysplastic syndromes, and indolent non-Hodgkin lymphoma. While early dose-escalation studies sponsored by Millennium Pharmaceuticals/Takeda were terminated, several Phase I trials sponsored by the National Cancer Institute continue to assess the agent's safety and tolerability. These ongoing evaluations encompass diverse recruitment statuses, ranging from active recruitment and suspended to not yet recruiting.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06223542	RECRUITING	Advanced Lymphoma; Advanced Malignant Solid Neoplasm; Indolent Non-Hodgkin Lymphoma; Metastatic Malignant Solid Neoplasm; Recurrent Malignant Solid Neoplasm; Refractory Malignant Solid Neoplasm	National Cancer Institute (NCI)	2025-03-24	PHASE1
NCT03816319	SUSPENDED	Myelodysplastic Syndrome With Excess Blasts; Recurrent Acute Myeloid Leukemia; Recurrent Myelodysplastic Syndrome; Recurrent Myelodysplastic Syndrome/Acute Myeloid Leukemia; Refractory Acute Myeloid Leukemia; Refractory Myelodysplastic Syndrome; Refractory Myelodysplastic Syndrome/Acute Myeloid Leukemia	National Cancer Institute (NCI)	2025-03-12	PHASE1
NCT03816319	Not yet recruiting	Myelodysplastic Syndrome\|Recurrent Acute Myeloid Leukemia\|Refractory Acute Myeloid Leukemia\|Refractory Chronic Myelomonocytic Leukemia\|Refractory High Risk Myelodysplastic Syndrome	National Cancer Institute (NCI)	2024-08-30	Phase 1
NCT02045095	TERMINATED	Advanced Malignant Solid Tumors	Millennium Pharmaceuticals, Inc.	2014-01-31	PHASE1
NCT02045095	Terminated	Advanced Malignant Solid Tumors	Millennium Pharmaceuticals Inc.\|Takeda	2014-01-31	Phase 1

(data from https://clinicaltrials.gov, updated on 2026-05-13)

Check the TAK-243 (MLN7243) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

TAK-243 selectively binds to and inhibits ubiquitin-activating enzyme, thereby disrupting downstream ubiquitin-conjugating E2 thioester bond formation and impairing global protein polyubiquitination. This inhibition triggers severe endoplasmic reticulum stress, abrogates nuclear factor kappa B pathway activation, and induces apoptosis, providing a mechanistic basis for tumor growth inhibition in clinical evaluations for advanced solid tumors, lymphomas, and acute myeloid leukemia.

Appendix RUO and cGMP Quality Standards

Quality Dimension	RUO (Research Use Only)	cGMP (Current Good Manufacturing Practice)
Clinical Applicability	Prohibited in human clinical trials or medical diagnostics.	Mandatory for human clinical trials (Phase I–III) and therapies.
Regulatory Status	Non-regulated grade; exempt from drug manufacturing laws.	Legally enforced by health authorities (e.g., FDA, EMA, NMPA).
Facility Environment	Unclassified analytical or research laboratories.	Validated Cleanrooms (ISO Class 5–8) with continuous monitoring.
Quality Control	Basic purity and activity testing.	Rigorous safety release testing (Sterility, Endotoxin, Mycoplasma).
Process Validation	Basic equipment calibration; no process validation required.	Full qualification (IQ/OQ/PQ) and complete batch records.
Quality Assurance	Vendor self-declared without required formal QMS.	Mandatory QA/QC unit, Change Control, CAPA, and vendor audits.
Regulatory Impact	High risk of IND rejection if used as a critical raw material.	Required for IND/NDA filings, supported by Drug Master Files (DMF).

Footnotes

Regulatory Note: Governed by FDA (21 CFR Parts 210/211/312), EMA (EudraLex Vol 4), ICH Guidelines (E6/Q7/Q9/Q10), and compendial standards (USP <71>/<85>/<1043>).