OBP-801

Histone Deacetylase (HDAC) Inhibitor (cyclic Depsipeptide)Rx: InvestigationalCompound: Investigational

Also known as: OBP801, Spiruchostatin B analogue, YM753

Educational Only — Not medical advice. Consult a qualified clinician before using any peptide.

Summary

OBP-801 (also known as YM753 or spiruchostatin B analog) is a cyclic depsipeptide HDAC inhibitor under investigation for solid tumors and hematologic malignancies. It has demonstrated potent antitumor activity in preclinical models, particularly against breast cancer and ovarian cancer, and has entered early-phase clinical trials in Japan and elsewhere.

Mechanism of Action

Selectively inhibits class I histone deacetylases (HDAC1, HDAC2, HDAC3, HDAC8), leading to hyperacetylation of histones, reactivation of silenced tumor suppressor genes, induction of cell cycle arrest, and apoptosis in cancer cells.

Routes of Administration

Intravenous

Goals & Uses

  • Combination anticancer therapyOncologyLow
  • Antitumor activity in solid tumorsOncologyModerate
  • Epigenetic reprogramming of cancer cellsOncology/EpigeneticsModerate
  • Hematologic malignancy treatmentOncologyLow

Contraindications

  • Severe hepatic impairmentOrganModerateLiver function concerns
  • Known hypersensitivity to cyclic depsipeptide HDAC inhibitorsAllergyHigh
  • Severe cardiac arrhythmia or QTc prolongationCardiovascularHigh

Adverse Effects

  • ThrombocytopeniaHematologicCommonLow platelet count
  • QTc prolongationCardiacUncommon
  • Nausea/vomitingGastrointestinalCommon
  • NeutropeniaHematologicUncommonLow neutrophil count
  • FatigueGeneralCommonLow energy or tiredness
  • Elevated liver enzymesHepaticUncommonIncrease in AST/ALT or other hepatic markers

Drug Interactions

  • Anticoagulants (e.g., warfarin)Moderate
  • QTc-prolonging agents (e.g., antiarrhythmics, certain antipsychotics)High
  • Strong CYP3A4 inhibitorsModerate

Population Constraints

  • PregnancyReproductive SafetyAbsolute
  • Severe renal impairmentOrgan ImpairmentRelative
  • Pediatric patientsAgeRelative
  • BreastfeedingReproductiveAbsolute

Regulatory Status

  • European UnionUnknownNo EMA approval; clinical activity primarily in Japan.
  • United StatesInvestigationalNo FDA approval; IND status not publicly confirmed; investigational use only.
  • United KingdomUnknownNo MHRA approval on record.

OBP-801 has been evaluated in Phase I clinical trials primarily in Japan. It does not hold approved status in any major jurisdiction as of the available data. It is a research/investigational compound.

Evidence & Sources

No sources recorded yet.

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