Immune Protocol
Bestatin (Ubenimex)Complete Dosing & Administration Guide
Natural dipeptide analogue aminopeptidase inhibitor with dual immunostimulatory and antitumor activity, approved in Japan as adjuvant cancer therapy
Dose Range
10-100mg
Frequency
Once daily
Route
Oral (capsule)
Cycle Length
12+ weeks
Dosing
How much
do I take?
Starting Dose
10-20 mg once daily
Start at the lower end to assess tolerance. Bestatin is well-tolerated orally, but beginning at 10-20 mg allows monitoring for gastrointestinal tolerance and any allergic reactions before increasing to the standard therapeutic dose. Take in the morning with or without food.
Standard Dose
30 mg once daily
The 30 mg once-daily dose is the standard therapeutic regimen used in Japanese clinical practice for leukemia maintenance. This dose has been validated in Phase 1 trials as providing optimal immunostimulatory effects with minimal side effects. Clinical trials in Japan demonstrated significant survival benefits at this dose when used after chemotherapy-induced complete remission in AML patients.
Advanced Dose
60-100 mg once daily
Higher doses of 60-100 mg daily have been explored in clinical trials, particularly for non-oncology indications such as pulmonary arterial hypertension. Phase 1 studies estimated the clinical optimal dose range as 10-100 mg daily. Higher doses should only be used under direct medical supervision, with monitoring of liver function and complete blood counts. The Phase 2 PAH trial (NCT02664558) used higher doses to achieve sufficient LTA4H inhibition for vascular benefit.
Timing
Best time to take
Take Bestatin (Ubenimex) at the same time each day for consistent blood levels. Morning dosing with breakfast is often preferred, but follow your healthcare provider's specific instructions.
With food?
Bestatin (Ubenimex) can typically be taken with or without food. Taking it with a light meal may help reduce any GI discomfort. Avoid taking with grapefruit juice or high-fat meals unless specifically directed.
If stacking
Bestatin (Ubenimex) should be used as directed by your healthcare provider. If combining with other medications or supplements, discuss potential interactions with your provider. Avoid combining with compounds that have overlapping mechanisms unless specifically guided by a medical professional.
Adjusting Your Dose
Increase if
- +You are being treated for pulmonary arterial hypertension under physician guidance and require higher LTA4H inhibition
- +Your oncologist recommends dose escalation based on insufficient immune response markers
- +You have tolerated the starting dose well and are transitioning to the standard therapeutic dose
Decrease if
- -You experience persistent gastrointestinal side effects at the current dose
- -Liver function tests show elevated transaminases above acceptable thresholds
- -You develop significant skin reactions or allergic symptoms
Signs of right dose
- ✓Stable or improving T-lymphocyte counts on blood work
- ✓Maintenance of complete remission in AML patients
- ✓Reduced frequency of infections during cancer treatment
- ✓Normal liver function tests during treatment
Dosing Calculator
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Administration
How do I
use it?
Reconstitution
What you need
- •Bestatin (Ubenimex) in its prescribed form
- •Clean, dry storage container
- •Measuring device if applicable (oral syringe, measuring cup)
- •Calendar or reminder app for dosing schedule
Injection
Route
Bestatin (Ubenimex) is administered Oral (capsule)—no injection required
Best sites
- •Not applicable—this is not an injectable formulation
Technique
- 1.Follow the specific administration instructions for your Bestatin (Ubenimex) formulation
- 2.Take or apply as directed by your healthcare provider
- 3.Store properly between uses according to package instructions
Storage
Signs of degradation
Sample Daily Schedule
Safety
Is it
safe?
Safety Profile
Bestatin (ubenimex) has an established safety profile based on decades of clinical use in Japan for AML maintenance therapy at 30 mg daily. The compound is generally well-tolerated, with the most common side effects being mild gastrointestinal symptoms and skin reactions. Japanese post-marketing surveillance and long-term clinical studies have not identified major safety concerns at standard doses. Phase 2 trials in the US for PAH and lymphedema also demonstrated acceptable safety profiles at higher doses.
Safety data is supported by Japanese regulatory approval, Phase 1-2 clinical trials, and decades of post-marketing surveillance. FDA orphan drug designation for PAH indicates adequate safety data for continued clinical development. Most safety data comes from Japanese clinical experience; data in non-Japanese populations is more limited.
Common Side Effects
Experienced by some users
Gastrointestinal discomfort
Mild nausea, diarrhea, or abdominal discomfort are the most frequently reported side effects with oral bestatin. These are typically transient and occur during the first week of treatment.
Management: Take with a small amount of food or water if stomach upset occurs. Symptoms usually resolve within a few days of continued use. If persistent, consider temporary dose reduction.
Skin rash or pruritus
Mild skin reactions including rash, itching, or urticaria have been reported in a subset of patients. These are generally mild and do not require discontinuation.
Management: Antihistamines may provide symptomatic relief. If rash is widespread or accompanied by systemic symptoms, discontinue and consult healthcare provider. Usually resolves within days of stopping treatment.
Facial flushing
Transient facial flushing or warmth may occur, particularly during the initial days of treatment, likely related to immune activation and histamine release.
Management: Usually self-limiting and resolves within 30-60 minutes of dosing. No treatment required. If persistent or bothersome, dose reduction may help.
Fatigue
Mild fatigue or malaise may occur as the immune system is stimulated. This is more commonly noted in patients concurrently receiving chemotherapy.
Management: Ensure adequate rest and hydration. Fatigue typically improves after the first 1-2 weeks of treatment. May be managed with dose timing adjustment to evening if daytime fatigue is problematic.
Less Common
- •Elevated liver enzymes
- •Mild leukopenia
These typically resolve with continued use or dose adjustment.
Stop and Seek Help If
- ×Severe allergic reaction (rash, swelling, difficulty breathing)
- ×Significant liver enzyme elevation (AST/ALT >3x upper limit of normal)
- ×Persistent or worsening side effects despite dose adjustment
- ×Disease relapse requiring change in treatment protocol
- ×Physician determines treatment goals have been achieved or treatment is no longer beneficial
Always consult with your healthcare provider before stopping bestatin, especially during cancer treatment. Abrupt discontinuation during AML maintenance therapy should only be done under medical supervision.
Interactions
With other peptides
- ✓Both enhance immune function through complementary mechanisms — Thymosin Alpha-1 promotes thymic T-cell maturation while bestatin enhances peripheral T-cell activation. Combination may provide synergistic immune support but should be monitored for excessive immune stimulation.
- ✓Complementary immune enhancement pathways. TP-5 modulates thymic function while bestatin acts on aminopeptidases. No known negative interactions, but combination has not been extensively studied.
- ✓BPC-157 focuses on tissue repair while bestatin targets immune function. No overlapping mechanisms or known interactions. Can likely be used concurrently without issues.
With medications
- ✓Chemotherapy agents (cytarabine, daunorubicin) - Bestatin is specifically designed and approved to be used alongside AML chemotherapy. Clinical trials demonstrated synergistic benefits with standard induction and maintenance regimens.
- !Immunosuppressants (cyclosporine, tacrolimus) - Bestatin's immunostimulatory effects directly counteract immunosuppressive therapy. Avoid concurrent use or use only with careful immune monitoring.
- !ACE inhibitors - Bestatin inhibits aminopeptidases involved in angiotensin metabolism, which may potentiate the hypotensive effects of ACE inhibitors. Monitor blood pressure closely if used together.
- ✓Antibiotics - No known negative interactions with common antibiotics. Bestatin may complement antibiotic therapy by enhancing immune clearance of infections.
With supplements
- ✓Vitamin D - Vitamin D supports immune function through complementary pathways and may enhance bestatin's immunostimulatory effects. Safe to combine.
- ✓Zinc - Zinc is essential for proper immune cell function and T-lymphocyte development. May complement bestatin's immune-enhancing effects. Safe to combine.
- ✓Green tea extract (EGCG) - EGCG has aminopeptidase inhibitory properties that may overlap with bestatin. While generally safe, combining multiple aminopeptidase inhibitors may lead to additive effects. Use with awareness.
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