Methoxsalen
Capsule, Liquid Filled · Oral
Uses
III. INDICATIONS AND USAGE Photochemotherapy (Methoxsalen with long wave UVA radiation) is indicated for the symptomatic control of severe, recalcitrant, disabling psoriasis not adequately responsive to other forms of therapy and when the diagnosis has been supported by biopsy. Methoxsalen is intended to be administered only in conjunction with a schedule of controlled doses of long wave ultraviolet radiation.
Dosage and administration
IX. DRUG DOSAGE & ADMINISTRATION CAUTION: Methoxsalen Capsules, USP represents a new dose form of methoxsalen. This new dosage form of methoxsalen exhibits significantly greater bioavailability and earlier photosensitization onset time than previous methoxsalen dosage forms. Each patient should be evaluated by determining the minimum phototoxic dose (MPD) and phototoxic peak time after drug administration prior to onset of photochemotherapy with this dosage form. Human bioavailability studies have indicated the following drug dosage and administration directions are to be used as a guideline only. PSORIASIS THERAPY 1. DRUG DOSAGE -INITIAL THERAPY: Methoxsalen capsules should be taken 1-1/2 to 2 hours before UVA exposure with some low-fat food or milk according to the following table: Patient's Weight Dose (kg) (lbs) (mg) <30 <66 10 30-50 66-110 20 51-65 112-143 30 66-80 146-176 40 81-90 179-198 50 91-115 201-254 60 >115 >254 70 Geriatric patients should generally be started at the low end of the dose recommended according to body weight and closely monitored during PUVA therapy. Although clinical experience has not identified differences in response between elderly and younger patients, the use of methoxsalen in older individuals may be affected by the presence of pre-existing medical conditions. 2. INITIAL EXPOSURE: The initial UVA exposure energy level and corresponding time of exposure is determined by the patient's skin characteristics for sun burning and tanning as follows: *Patients with natural pigmentation of these types should be classified into a lower skin type category if the sunburning history so indicates. Skin Type History Recommended J/cm 2 I Always burn, never tan (patients with erythrodermic psoriasis are to be classed as Type I for determination of UVA dosage.) 0.5 J/cm 2 II Always burn, but sometimes tan 1.0 J/cm 2 III Sometimes burn, but always tan 1.5 J/cm 2 IV Never burn, always tan 2.0 J/cm 2 Skin Type Physician Examination J/cm 2 V* Moderately pigmented 2.5 J/cm 2 VI* Blacks 3.0 J/cm 2 If the MPD is done, start at 1/2 MPD. Additional drug dosage directions are as follows: Weight Change: In the event that the weight of a patient changes during treatment such that he/she falls into an adjacent weight range/dose category, no change in the dose of methoxsalen is usually required. If, in the physician's opinion, however, a weight change is sufficiently great to modify the drug dose, then an adjustment in the time of exposure to UVA should be made. Dose/Week: The number of doses per week of methoxsalen capsules will be determined by the patient's schedule of UVA exposures. In no case should treatments be given more often than once every other day because the full extent of phototoxic reactions may not be evident until 48 hours after each exposure. Dosage Increase: Dosage may be increased by 10 mg. after the 15th treatment under the conditions outlined in section XI.B.4.b. X. UVA RADIATION SOURCE SPECIFICATIONS AND INFORMATION A. IRRADIANCE UNIFORMITY The following specifications should be met with the window of the detector held in a vertical plane: Vertical Variation: For readings taken at any point along the vertical center axis of the chamber (to within 15 cm from the top and bottom), the lowest reading should not be less than 70 % of the highest reading. Horizontal Variation: Throughout any specific horizontal plane, the lowest reading must be at least 80 % of the highest reading, excluding the peripheral 3 cm of the patient treatment space. B. PATIENT SAFETY FEATURES: The following safety features should be present: (1) Protection from electrical hazard: All units should be grounded and conform to applicable electrical codes. The patient or operator should not be able to touch any live electrical parts. There should be ground fault protection. (2) Protective shielding of lamps: The patient should not be able to come in contact with the bare lamps. In the event of lamp breakage, the patient should not be exposed to broken lamp components. (3) Hand rails and hand holds: Appropriate supports should be available to the patient. (4) Patient viewing window: A window which blocks UV should be provided for viewing the patient during treatment. (5) Door and latches: Patients should be able to open the door from the inside with only slight pressure to the door. (6) Non-skid floor: The floor should be of a non-skid nature. (7) Thermoregulation: Sufficient air flow should be provided for patient safety and comfort, limiting temperature within the UVA radiator cabinet to approximately less than 100 °F. (8) Timer: The irradiator should be equipped with an automatic timer which terminates the exposure at the conclusion of a pre-set time interval. (9) Patient alarm device: An alarm device within the UVA irradiator chamber should be accessible to the patient for emergency activation. (10) Danger label: The unit should have a label prominently displayed which reads as follows: DANGER - Ultraviolet radiation - Follow your physicians instructions - Failure to use protective eyewear may result in eye injury. C. UVA EXPOSURE DOSIMETRY MEASUREMENTS: The maximum radiant exposure or irradiance (within ±15%) of UVA (320-400 nm) delivered to the patient should be determined by using an appropriate radiometer calibrated to be read in J/cm 2 or mW/cm 2 . In the absence of a standard measuring technique approved by the National Bureau of Standards, the system should use a detector corrected to a cosine spatial response. The use and recalibration frequency of such a radiometer for a specific UVA irradiator chamber should be specified by the manufacturer because the UVA dose (exposure) is determined by the design of the irradiator, the number of lamps, and the age of the lamp. If irradiance is measured, the radiometer reading in mW/cm 2 is used to calculate the exposure time in minutes to deliver the required UVA in J/cm 2 to a patient in the UVA irradiator cabinet.
Contraindications
IV. CONTRAINDICATIONS A. Patients exhibiting idiosyncratic reactions to psoralen compounds. B. Patients possessing a specific history of light sensitive disease states should not initiate methoxsalen therapy except under special circumstances. Diseases associated with photosensitivity include lupus erythematosus, porphyria cutanea tarda, erythropoietic protoporphyria, variegate porphyria, xeroderma pigmentosum, and albinism. C. Patients with melanoma or with a history of melanoma. D. Patients with invasive squamous cell carcinomas. E. Patients with aphakia, because of the significantly increased risk of retinal damage due to the absence of lenses.
Warnings
V. WARNINGS - GENERAL A. SKIN BURNING: Serious burns from either UVA or sunlight (even through window glass) can result if the recommended dosage of the drug and/or exposure schedules are exceeded. B. CARCINOGENICITY: ANIMAL STUDIES: Topical or intraperitoneal methoxsalen has been reported to be a potent photocarcinogen in albino mice and hairless mice (Hakim et al., 1960 10 ). However, methoxsalen given by the oral route to Swiss albino mice suggests this agent exerts a protective effect against ultraviolet carcinogenesis; mice given 8-methoxypsoralen in their diet showed 38% ear tumors 180 days after the start of ultraviolet therapy compared to 62% for controls (O'Neal et al., 1957 11 ). HUMAN STUDIES: A 5.7 year prospective study of 1380 psoriasis patients treated with oral methoxsalen and ultraviolet A photochemotherapy (PUVA) demonstrated that the risk of cutaneous squamous-cell carcinoma developing at least 22 months following the first PUVA exposure was approximately 12.8 times higher in the high dose patients than in the low dose patients (Stern et al., 1979 12 , Stern et al., 1980 13 , and Stern et al., 1984 14 ). The substantial dose-dependent increase was observed in patients with neither a prior history of skin cancer nor significant exposure to cutaneous carcinogens. Reduction in PUVA dosage significantly reduces the risk. No substantial dose-related increase was noted for basal cell carcinoma according to Stern et al., 1984 14 . Increases appear greatest in patients who have pre-PUVA exposure to 1) prolonged tar and UVB treatment, 2) ionizing radiation, or 3) arsenic. Roenigk et al., 1980 15 , studied 690 patients for up to 4 years and found no increase in the risk of non-melanoma skin cancer, although patients in this cohort had significantly less exposure to PUVA than in the Stern et al. study. Recent analysis of new data in the Stern et al cohort (Stern et al., 1997 16 ) has shown that these patients have an elevated relative risk of contracting melanoma. The relative risk for melanoma in these patients was 2.3 (95% confidence interval 1.1 to 4.1). The risk is particularly higher in those patients who have received more than 250 PUVA treatments and in those whose treatment has spanned greater than 15 years earlier. Some patients developing melanoma did so even after having ceased PUVA therapy over 5 years earlier. These observations indicate the need for monitoring of PUVA patients for skin tumors throughout their lives. In a study in Indian patients treated for 4 years for vitiligo, 12% developed keratoses, but not cancer, in the depigmented, vitiliginous areas (Mosher, 1980 17 ). Clinically, the keratoses were keratotic papules, actinic keratosis-like macules, nonscaling dome-shaped papules, and lichenoid porokeratotic-like papules. C. CATARACTOGENICITY: ANIMAL STUDIES: Exposure to large doses of UVA causes cataracts in animals, and this effect is enhanced by the administration of methoxsalen (Cloud et al., 1960 18 ; Cloud et al., 1961 19 Freeman et al., 1969 20 ). HUMAN STUDIES: It has been found that the concentration of methoxsalen in the lens is proportional to the serum level. If the lens is exposed to UVA during the time methoxsalen is present in the lens, photochemical action may lead to irreversible binding of methoxsalen to proteins and the DNA components of the lens (Lerman et al., 1980 21 ). However, if the lens is shielded from UVA, the methoxsalen will diffuse out of the lens in a 24-hour period (Lerman et al., 1980 21 ). Patients should be told emphatically to wear UVA absorbing, wrap-around sunglasses for the 24-hour period following ingestion of methoxsalen whether exposed to direct or indirect sunlight in the open or through a window glass. Among patients using proper eye protection, there is no evidence for a significantly increased risk of cataracts in association with PUVA therapy (Stern et al., 1979 12 ). Thirty-five of 1380 patients have developed cataracts in the 5 years since their first PUVA treatment. This incidence is comparable to that expected in a population of this size and age distribution. No relationship between PUVA dose and cataract risk in this group has been noted. D. ACTINIC DEGENERATION: Exposure to sunlight and/or ultraviolet radiation may result in "premature aging" of the skin. E. BASAL CELL CARCINOMAS: Patients exhibiting multiple basal cell carcinomas or having a history of basal cell carcinomas should be diligently observed and treated. F. RADIATION THERAPY: Patients having a history of previous x-ray therapy or grenz ray therapy should be diligently observed for signs of carcinoma. G. ARSENIC THERAPY: Patients having a history of previous arsenic therapy should be diligently observed for signs of carcinoma. H. HEPATIC DISEASES: Patients with hepatic insufficiency should be treated with caution since hepatic biotransformation is necessary for drug urinary excretion. I. CARDIAC DISEASES: Patients with cardiac diseases or others who may be unable to tolerate prolonged standing or exposure to heat stress should not be treated in a vertical UVA chamber. J. GERIATRIC PATIENTS: Caution should be used in elderly patients, especially those with a pre-existing history of cataracts, cardiovascular conditions, kidney and/or liver dysfunction, or skin cancer. K. TOTAL DOSAGE: The total cumulative dose of UVA that can be given over long periods of time with safety has not as yet been established. L. CONCOMITANT THERAPY: Special care should be exercised in treating patients who are receiving concomitant therapy (either topically or systemically) with known photosensitizing agents such as anthralin, coal tar or coal tar derivatives, griseofulvin, phenothiazines, nalidixic acid, fluoroquinolone antibiotics, halogenated salicylanilides (bacteriostatic soaps), sulfonamides, tetracyclines, thiazides and certain organic staining dyes such as methylene blue, toluidine blue, rose bengal, and methyl orange.
Precautions
VI. PRECAUTIONS A. GENERAL - APPLICABLE TO PSORIASIS TREATMENT: BEFORE METHOXSALEN INGESTION Patients must not sunbathe during the 24 hours prior to methoxsalen ingestion and UV exposure. The presence of a sunburn may prevent an accurate evaluation of the patient's response to photochemotherapy. AFTER METHOXSALEN INGESTION UVA-absorbing wrap-around sunglasses should be worn during daylight for 24 hours after methoxsalen ingestion. The protective eyewear must be designed to prevent entry of stray radiation to the eyes, including that which may enter from the sides of the eyewear. The protective eyewear is used to prevent the irreversible binding of methoxsalen to the proteins and DNA components of the lens. Cataracts form when enough of the binding occurs. Visual discrimination should be permitted by the eyewear of patient well-being and comfort. Patients must avoid sun exposure, even through window glass or cloud cover, for at least 8 hours after methoxsalen ingestion. If sun exposure cannot be avoided, the patient should wear protective devices such as a hat and gloves, and/or apply sunscreens which contain ingredients that filter out UVA radiation (e.g., sunscreens containing benzophenone and/or PABA esters which exhibit a sun protective factor equal to or greater than 15). These chemical sunscreens should be applied to all areas that might be exposed to the sun (including lips). Sunscreens should not be applied to areas affected by psoriasis until after the patient has been treated in the UVA chamber. DURING PUVA THERAPY Total UVA-absorbing/blocking goggles mechanically designed to give maximal ocular protection must be worn. Failure to do so may increase the risk of cataract formation. A reliable radiometer can be used to verify elimination of UVA transmission through the goggles. Abdominal skin, breasts, genitalia, and other sensitive areas should be protected for approximately 1/3 of the initial exposure time until tanning occurs. Unless affected by disease, male genitalia should be shielded. AFTER COMBINED METHOXSALEN/UVA THERAPY UVA-absorbing wrap-around sunglasses should be worn during daylight for 24 hours after combined methoxsalen/UVA therapy. Patients should not sunbathe for 48 hours after therapy. Erythema and/or burning due to photochemotherapy and sunburn due to sun exposure are additive.
Side effects
VII. ADVERSE REACTIONS: A. METHOXSALEN: The most commonly reported side effect of methoxsalen alone is nausea, which occurs with approximately 10% of all patients. This effect may be minimized or avoided by instructing the patient to take methoxsalen in milk or food, or to divide the dose into two portions, taken approximately one-half hour apart. Other effects include nervousness, insomnia, and depression. B. COMBINED METHOXSALEN/UVA THERAPY: PRURITUS: This adverse reaction occurs with approximately 10% of all patients. In most cases, pruritus can be alleviated with frequent application of bland emollients or other topical agents; severe pruritus may require systemic treatment. If pruritus is unresponsive to these measures, shield pruritic areas from further UVA exposure until the condition resolves. If intractable pruritus is generalized, UVA treatment should be discontinued until the pruritus disappears. ERYTHEMA: Mild, transient erythema at 24-48 hours after PUVA therapy is an expected reaction and indicates that a therapeutic interaction between methoxsalen and UVA occurred. Any area showing moderate erythema (greater than Grade 2 - See Table 1 for grades of erythema) should be shielded during subsequent UVA exposures until the erythema has resolved. Erythema greater than Grade 2 which appears within 24 hours after UVA treatment may signal a potentially severe burn. Erythema may become progressively worse over the next 24 hours, since the peak erythemal reaction characteristically occurs 48 hours or later after methoxsalen ingestion. The patient should be protected from further UVA exposures and sunlight, and should be monitored closely. IMPORTANT DIFFERENCES BETWEEN PUVA ERYTHEMA AND SUNBURN: PUVA-induced inflammation differs from sunburn or UVB phototherapy in several ways. The % transmission of UVB varies between 0% to 34% through skin whereas UVA varies between 1% to 80% transmission; thus, UVA is transmitted to a larger % through the skin. (Diffey, 1982 22 ). The DNA lesions induced by PUVA are very different from UV-induced thymine dimers and may lead to a DNA crosslink. This DNA lesion may be more problematic to the cell because crosslinks are more lethal and psoralen-DNA photoproducts may be "new" or unfamiliar substrates for DNA repair enzymes. DNA synthesis is also suppressed longer after PUVA. The time course of delayed erythema is different with PUVA and may not involve the usual mediators seen in sunburn. PUVA-induced redness may be just beginning at 24 hours, when UVB erythema has already passed its peak. The erythema dose-response curve is also steeper for PUVA. Compared to equally erythemogenic doses of UVB, the histologic alterations induced by PUVA show more dermal vessel damage and longer duration of epidermal and dermal abnormalities. OTHER ADVERSE REACTIONS: Those reported include edema, dizziness, headache, malaise, depression, hypopigmentation, vesiculation and bullae formation, non-specific rash, herpes simplex, miliaria, urticaria, folliculitis, gastrointestinal disturbances, cutaneous tenderness, leg cramps, hypotension, and extension of psoriasis. To report SUSPECTED ADVERSE REACTION, contact Strides Pharma, Inc. at 1-877-244-9825 or go to www.strides.com or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
Drug interactions
D. DRUG INTERACTIONS: See WARNINGS – GENERAL.
Pregnancy
F. PREGNANCY: Animal reproduction studies have not been conducted with methoxsalen. It is also not known whether methoxsalen can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Methoxsalen should be given to a woman with reproductive capacity only if clearly needed.
Pediatric use
H. PEDIATRIC USE: Safety in children has not been established. Potential hazards of long-term therapy include the possibilities of carcinogenicity and cataractogenicity as described in the WARNINGS - GENERAL section as well as the probability of actinic degeneration which is also described in the WARNINGS - GENERAL Section.
Geriatric use
I. GERIATRIC USE: Clinical studies with Methoxsalen Capsules, USP 10 mg [Soft Gelatin Capsules] did not include sufficient numbers of subjects aged 65 and over to determine whether elderly subjects responded differently from younger subjects. Other reported clinical experience has not identified differences in response between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Overdosage
VIII. OVERDOSAGE In the event of methoxsalen overdosage, induce emesis and keep the patient in a darkened room for at least 24 hours. Emesis is most beneficial within the first 2 to 3 hours after ingestion of methoxsalen, since maximum blood levels are reached by this time.
Description
I. DESCRIPTION Methoxsalen Soft Gelatin Capsules USP contains 10mg methoxsalen. Methoxsalen occurs as white to pale yellow crystals and can be obtained naturally from seeds of Ammi majus and roots of Heracleum Candicans or through synthesis. Methoxsalen is practically insoluble in water, freely soluble in chloroform, soluble in boiling alcohol, in acetone, in acetic acid, in propylene glycol, and in benzene, sparingly soluble in boiling water and in ether. The chemical name of methoxsalen is 9-methoxy-7H-furo [3,2-g] [1] benzopyran-7-one; its empirical formula is C 12 H 8 O 4 and the molecular weight is 216.19. The structural formula is: Methoxsalen Capsules are available as soft gelatin capsules containing the following inactive ingredients: Citric acid anhydrous, D & C yellow 10, FD & C blue 1, Gelatin, Glycine, Glycerin, Isopropyl alcohol, Medium chain triglyceride, Polyethylene glycol 400, Polysorbate 80, Purified water, Titanium dioxide and Opacode black. The opacode black contains Propylene glycol, Shellac glaze (Modified) IN SD-45, N-Butyl alcohol, Black iron oxide, Isopropyl alcohol and Ammonium hydroxide. Methoxsalen
How supplied
XII. HOW SUPPLIED Methoxsalen Capsules, USP 10 mg is green color, oval shaped soft gelatin capsule imprinted with 'M10' containing no drug crystals and clear colorless to pale yellow liquid, each containing 10 mg of methoxsalen (8-methoxypsoralen). It is packed in amber colored glass bottles as 50's count (NDC 64380-752-16). Store at 20° to 25 °C (68° to 77 °F); excursions permitted between 15 °C - 30 °C (59 °F - 86 °F). [See USP Controlled Room Temperature] Distributed by: Strides Pharma, Inc. Bridgewater, NJ 08807
Patient information
B. INFORMATION FOR PATIENTS: See accompanying Patient Package Insert.
Label text from the FDA structured product label by Strides Pharma Science Limited (revised Jun 24, 2026). Long sections are shortened; the complete label is on DailyMed.
Active ingredients
- Methoxsalen in 1 product
Methoxsalen NDC products (1)
| NDC | Strength & form | Labeler | Type |
|---|---|---|---|
| 64380-752 | Methoxsalen 10 mg/1 Capsule, Liquid Filled | Strides Pharma Science Limited | ANDA |
Methoxsalen recalls
- D-0260-2024 Jan 31, 2024 · Class II · Terminated
Failed Dissolution Specifications
Frequently asked questions
What is Methoxsalen used for?
III. INDICATIONS AND USAGE Photochemotherapy (Methoxsalen with long wave UVA radiation) is indicated for the symptomatic control of severe, recalcitrant, disabling psoriasis not adequately responsive to other forms of therapy and when the diagnosis has been supported by biopsy. Methoxsalen is intended to be administered only in conjunction with a schedule of controlled doses of long wave…
What are the side effects of Methoxsalen?
VII. ADVERSE REACTIONS: A. METHOXSALEN: The most commonly reported side effect of methoxsalen alone is nausea, which occurs with approximately 10% of all patients. This effect may be minimized or avoided by instructing the patient to take methoxsalen in milk or food, or to divide the dose into two portions, taken approximately one-half hour apart. Other effects include nervousness, insomnia, and… See the full label for the complete list.
Who makes Methoxsalen?
Methoxsalen is listed by 1 labeler in the FDA NDC directory, including Strides Pharma Science Limited.
Has Methoxsalen been recalled?
The FDA enforcement database lists 1 recall for Methoxsalen, most recently D-0260-2024 (class ii): Failed Dissolution Specifications