Aminolevulinic Acid

ALA occurs endogenously as a metabolite that is formed in the mitochondria from succinyl-CoA and glycine. Exogenous administration of ALA leads to accumulation of the ALA metabolite PpIX in tumor cells.

• Gleolan is indicated in patients with glioma [suspected World Health Organization (WHO) Grades III or IV on preoperative imaging] as an adjunct for the visualization of malignant tissue during surgery. Gleolan is an optical imaging agent indicated in patients with glioma (suspected World Health Organization Grades III or IV on preoperative imaging) as an adjunct for the visualization of malignant tissue during surgery.

• Hypersensitivity to the aminolevulinic acid (ALA) or porphyrins. [see Warnings and Precautions (5.3) ] Acute or chronic types of porphyria, due to potential ineffectiveness of the drug in these patients.contraindicated

For oral use only ( 2.1 ) Recommended reconstituted oral dose of Gleolan is 20 mg/kg. ( 2.1 ) Administer Gleolan to patient orally 3 hours (range 2 to 4 hours) before anesthesia. ( 2.1 ) See Full Prescribing Information for reconstitution information. ( 2.2 ) Use appropriate visualization techniques with appropriate surgical microscopes and light source filters. ( 2.4 ) 2.1 Recommended Dose For oral use only The recommended oral dose of reconstituted Gleolan is 20 mg / kg body weight. More than 1 vial may be required. 2.2 Reconstitution of Gleolan Gleolan powder must be reconstituted prior to administration by a healthcare provider according to the following instructions: Determine the total number of vials needed to achieve the intended dose for the patient according to the equation below (rounded up to the nearest whole vial): # of vials = Patient Body Weight (kg) 75 kg / vial Completely remove the white cap and aluminum crimp seal from each vial. Remove and retain the rubber stopper from the vial. Using an appropriate volumetric measuring device (e.g., flask, graduated cylinder, dosing syringe), measure 50 mL of drinking water and add to each vial containing 1,500 mg of Gleolan. Gently swirl the vial to completely dissolve the powder. The resulting reconstituted solution (30 mg of Gleolan per mL) is clear and colorless to slightly yellowish. If required, replace the stopper and store reconstituted solution for up to 24 hours at room temperature prior to administration. 2.3 Gleolan Administration Gleolan is for ORAL USE ONLY.

Phototoxic reactions: Do not administer phototoxic drugs (St. John's wort, griseofulvin, thiazide diuretics, sulfonylureas, phenothiazines, sulphonamides, quinolones and tetracyclines), and topical preparations containing ALA for 24 hours during the perioperative period. Reduce exposure to sunlight or room lights for 48 hours after oral administration of Gleolan. ( 5.1 , 7 ) Risk of misinterpretation: Non-fluorescing tissue in the surgical field does not rule out the presence of tumor. ( 5.2 , 14 ) 5.1 Risk of Phototoxic Reaction Due to the risk of phototoxic reactions, do not administer phototoxic drugs (St. John's wort, griseofulvin, thiazide diuretics, sulfonylureas, phenothiazines, sulphonamides, quinolones and tetracyclines), and topical preparations containing ALA for 24 hours during the perioperative period [see Drug Interactions (7) ] . Reduce exposure to sunlight or room lights for 48 hours after administration of Gleolan. 5.2 Risk of Misinterpretation Errors may occur with the use of Gleolan for intraoperative visualization of malignant glioma, including false negatives and false positives. Non-fluorescing tissue in the surgical field does not rule out the presence of tumor in patients with glioma [see Clinical Studies (14) ] . Fluorescence may be seen in areas of inflammation or metastases from other tumor types. 5.3 Hypersensitivity Reactions Hypersensitivity reactions, including serious hypersensitivity reactions have occurred; these reactions include anaphylactic shock, swelling, and urticaria [see Contraindications (4) , Adverse Reactions (6.2) ] .

Adverse reactions occurring in >1% of patients in the week following surgery were pyrexia, hypotension, nausea, and vomiting. ( 6.1 ) Adverse reactions occurring in < 1% of patients in the first 6 weeks after surgery were: chills, photosensitivity reaction, solar dermatitis, hypotension, abnormal liver function test, and diarrhea. ( 6.1 ) Neurologic events related to the surgical procedure occurred in 29% of patients and included: aphasia, hemiparesis, hemianopia, headache, seizure, hemiplegia, monoparesis, hypoesthesia, and brain edema. ( 6.1 ) Elevated liver enzymes occurred in clinical studies. There were no cases of liver failure. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact NXDC toll-free at (844) 517-5252 and adverseevents@nxdevcorp.com or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trial Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of Gleolan is supported by data from 5 open label clinical studies, which included 527 patients with glioma who received ALA HCl. Adverse reactions that occurred in > 1% of patients in the week following surgery were pyrexia, hypotension, nausea, and vomiting. Adverse reactions occurring in the first 6 weeks after surgery in < 1% of patients were: chills, photosensitivity reaction, solar dermatitis, hypotension, abnormal liver function test, and diarrhea.

8.1 Pregnancy Risk Summary There are no available human data on Gleolan in pregnant women to inform a drug associated risk of adverse developmental outcomes. In animal reproduction studies, no adverse developmental effects were observed with oral ALA HCl administration to pregnant rabbits during organogenesis at doses 3 times the maximum recommended human oral dose (see Data ) . The estimated background risk of major birth defects and miscarriage for the indicated populations are unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. Animal data ALA HCl was administered to rabbits at oral doses of 15, 50 and 150 mg/kg/day [approximately 0.1, 0.6, and 3 times the maximum human recommended dose (MHRD), respectively based on AUC comparisons] from gestation days 6-18. The no-observed-adverse-effect level (NOAEL) for maternal toxicity was 50 mg/kg/day and the NOAEL for embryo-fetal developmental toxicity was 150 mg/kg/day. 8.2 Lactation Risk summary There are no data on the presence of ALA HCl in either human or animal milk, the effects on the breastfed infant, or the effects on milk production.

Metabolism

In 12 healthy subjects, the mean half-life of ALA following the recommended dose of Gleolan solution was 0.9 ± 1.2 hours (mean ± std dev) with a range of 0.8 to 1.3 hours. Maximum concentrations of the PpIX metabolite (T max for PpIX) occurred with a median of 4 hours and a range of 1.2 to 7.8 hours.

Overdosage has been associated with respiratory insufficiency and erythema. In the event of overdose, supportive measures should be provided as necessary, including protection from strong light sources.

• Dec 3, 1999NDANDA020965Sun Pharm Inds Inc
• May 10, 2016NDANDA208081Biofrontera
• Jun 6, 2017NDANDA208630Nxdc

1. 1Drug Ineffective30718%
2. 2Wrong Technique In Product Usage Process18211%
3. 3Poor Quality Product Administered17710%
4. 4Product Quality Issue1538.8%
5. 5Off Label Use1498.6%
6. 6Erythema1166.7%
7. 7Product Dose Omission Issue1146.6%
8. 8Application Site Pain945.4%
9. 9Application Site Erythema844.9%
10. 10Accidental Exposure To Product804.6%
11. 11Pain754.3%
12. 12Product Physical Issue623.6%
13. 13Blister523.0%
14. 14Eye Irritation362.1%
15. 15Skin Exfoliation362.1%

Recent PubMed references pinned to Aminolevulinic Acid as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Radiodynamic Therapy Using 5-Aminolevulinic Acid as a New Treatment Option for Osteosarcoma: An In Vitro and In Vivo Study.
  Anticancer research · 2026 · Tanemura Y, Nakamura T, Matsuyama Y, et al.
  PMID 42203311DOI 10.21873/anticanres.18183
• Photodynamic and antibiotic combination therapy against multidrug-resistant Pseudomonas aeruginosa wound infections in diabetic rats.
  Bioorganic chemistry · 2026 · Kong F, Zhang T, Liu Y, et al.
  PMID 42127741DOI 10.1016/j.bioorg.2026.109955
• Safety and Efficacy of Aminolevulinic Acid 20% Topical Solution Activated by Blue Light for Facial Cutaneous Squamous Cell Carcinoma in situ.
  Journal of drugs in dermatology : JDD · 2026 · Nestor MS, Chaudry A, Vanaria RJ, et al.
  PMID 42081635DOI 10.36849/JDD.9192
• Capsaicin ameliorates glycemic levels via gut microbiota-derived 5-aminolevulinic acid in mice.
  Microbiome · 2026 · Fang Q, Huang S, Zhang C, et al.
  PMID 42067917DOI 10.1186/s40168-026-02415-8
• Derivatives of ALA as theranostic agents for photodynamic therapy and fluorescence imaging of peritoneal dissemination of ovarian cancer.
  Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2026 · Céspedes M, Orlando CG, Calvo G, et al.
  PMID 42061135DOI 10.1016/j.biopha.2026.119435
• Theranostic CuS/ALA Nanoprobes Modulate Drug Efflux Pumps and Synergize the Photoacoustics-Guided Photothermal Breast Cancer Therapy.
  ACS applied materials & interfaces · 2026 · Parihar N, Patil PM, Sen S, et al.
  PMID 42013020DOI 10.1021/acsami.6c01676
• Effects of 5 aminolevulinic acid on fruit quality and volatile metabolites of Meizao sweet cherry.
  Scientific reports · 2026 · Guo H, Zhang J, Wang H, et al.
  PMID 41998214DOI 10.1038/s41598-026-49051-8
• Drug-resistant clinical Candida responded to 5-aminolevulinic acid photodynamic therapy (ALA-PDT) in vitro via enhanced ROS release.
  Antimicrobial agents and chemotherapy · 2026 · Yang Z, Zhang Y, Li D, et al.
  PMID 41996174DOI 10.1128/aac.01645-25

The 10 most recently updated of 293 ClinicalTrials.gov registrations naming Aminolevulinic Acid as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Fluorescence Image Guided Surgery Followed by Intraoperative Photodynamic Therapy for Improving Local Tumor Control in Patients With Locally Advanced or Recurrent Colorectal Cancer
  Recruiting · Phase 1 · Phase 2 · Interventional · 21 enrolled · Roswell Park Cancer Institute
  NCT06307548updated 2026-06-05
• Adjuvant Temozolomide ± 5-Aminolevulinic Acid + Low Intensity Diffuse Ultrasound Sonodynamic Therapy System for Newly Diagnosed Glioblastoma
  Recruiting · Phase 2 · Interventional · 103 enrolled · Alpheus Medical, Inc.
  NCT07225621updated 2026-06-05
• Loupe-Based Intraoperative Fluorescence Imaging
  Recruiting · Observational · 30 enrolled · Guoqiang Yu
  NCT04780009updated 2026-06-03
• PD L 506 for Stereotactic Interstitial Photodynamic Therapy of Newly Diagnosed Supratentorial IDH Wild-type Glioblastoma
  Terminated · Phase 2 · Interventional · 17 enrolled · photonamic GmbH & Co. KG
  NCT03897491updated 2026-06-01
• Alteration of the Immune Microenvironment in Basal Cell Carcinoma Following Photodynamic Therapy
  Active not recruiting · Phase 2 · Interventional · 18 enrolled · Case Comprehensive Cancer Center
  NCT05020912updated 2026-06-01
• Study to Evaluate the Safety, Tolerability and Efficacy of BF-200 ALA (Ameluz®) in the Field-directed Treatment of Actinic Keratosis (AK) on the Extremities and Neck/Trunk With Photodynamic Therapy (PDT) Using a RhodoLED Lamp
  Active not recruiting · Phase 3 · Interventional · 172 enrolled · Biofrontera Inc.
  NCT05662202updated 2026-05-22
• Phase I Study in Advanced Malignancies With 5-ALA
  Suspended · Phase 1 · Interventional · 130 enrolled · Fox Chase Cancer Center
  NCT04381806updated 2026-05-22
• A Dose-escalation Clinical Study of Intraoperative Photodynamic Therapy of Glioblastoma
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 12 enrolled · Hemerion Therapeutics
  NCT05736406updated 2026-05-22
• Gleolan for Visualization of Newly Diagnosed or Recurrent Meningioma
  Completed · Phase 3 · Interventional · 108 enrolled · NX Development Corp
  NCT04305470updated 2026-05-18
• Longitudinal Study of the Porphyrias
  Recruiting · Observational · 1,500 enrolled · The American Porphyrias Expert Collaborative
  NCT01561157updated 2026-05-15

Frequently asked questions

How does Aminolevulinic Acid work?

ALA occurs endogenously as a metabolite that is formed in the mitochondria from succinyl-CoA and glycine. Exogenous administration of ALA leads to accumulation of the ALA metabolite PpIX in tumor cells.

What is Aminolevulinic Acid used for?

According to FDA labeling, Aminolevulinic Acid carries indications including: Gleolan is indicated in patients with glioma [suspected World Health Organization (WHO) Grades III or IV on preoperative imaging] as an adjunct for the visualization of malignant tissue during surgery. Gleolan is an optical imaging agent indicated in patients with glioma (suspected World Health Organization Grades III or IV on preoperative imaging) as an adjunct for the visualization of malignant tissue during surgery.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Aminolevulinic Acid?

Aminolevulinic Acid is classified as Sensitizers used in photodynamic/radiation therapy, Optical Imaging Agent, Porphyrin Precursor, Enzyme Interactions, Fluorescence Contrast Activity, Photosensitizing Activity.

What are the brand names for Aminolevulinic Acid?

Aminolevulinic Acid is marketed under brand names including Ameluz.

What are the contraindications for Aminolevulinic Acid?

Aminolevulinic Acid labeling lists contraindications including: Hypersensitivity to the aminolevulinic acid (ALA) or porphyrins. [see Warnings and Precautions (5.3) ] Acute or chronic types of porphyria, due to potential ineffectiveness of the drug in these patients.. Always consult the full prescribing information and a clinician.