Vitamin D Analogues Clinically Useful for Several Conditions


Calcium Regulation
Calcium regulation in the human body. The role of vitamin D is shown in orange.

There are several active pharmaceutical ingredient products known as vitamin D analogues, which are derivatives of this powerful vitamin, designed to aid patients’ health and well being. Vitamin D is known by many people as the vitamin that helps to create strong bones, but this is just one of the benefits of vitamin D. As a key regulator of serum calcium levels, vitamin D is detected by bone and intestinal cell receptors, thus regulating the level of calcium in the blood stream while determining how much should be stored in the skeleton. This regulation is crucial, as calcium is responsible for a variety of physiological processes, not just building bone. A lack of vitamin D can be devastating, and promote the breakdown of bones in conditions such as rickets in children, and osteomalacia, a softening of bones leading to an increased risk of fracture, in adults. Vitamin D affects the immune system by interacting with some types of cells to dampen the immune response. This can be beneficial in cases where the immune system is over-reactive, as in autoimmune diseases including type 1 diabetes, multiple sclerosis and rheumatoid arthritis. Some studies have found that people living in regions with more sunlight have lower rates of these diseases, but it is not clear whether higher vitamin D levels are responsible.

The following vitamin D analogues are all calcium regulators, designed to increase blood calcium levels in patients:


Calcitriol, CAS number 32222-06-3
calcitriolCalcitriol, CAS number 32222-06-3 is a calcium regulator, which increases blood calcium levels by promoting the absorption of dietary calcium from the gastrointestinal tract. Calcitriol additionally aids the body in increasing the reabsorption of calcium, therefore reducing the loss of calcium in the urine. Bone cells referred to as osteoclasts are stimulated via this release of calcium from the bone when patients take calcitriol, and intestinal absorption of both calcium and phosphorus is increased as well. Known as the injectable drug Calcijex, marketed by Abbott Laboratories, calcitriol is earmarked for use in the management of hypocalcemia in patients undergoing chronic renal dialysis.

Alfacalcidol CAS number 41294-56-8
AlfacalcidolAlfacalcidol CAS number 41294-56-8 (or 1-hydroxycholecalciferol) has less of an effect on calcium metabolism than calcitriol, while having more potent effects on parathyroid hormone levels and immune system, including regulatory T cells. Alfacalcidol, an analogue of vitamin D, is used to heal bone fractures and to treat metabolic bone diseases by inhibiting bone resorption and/or favor bone mineralization and bone regeneration. It is available in capsules, oral drops and injection form.

Calcifediol, CAS number 19356-17-3
Calcifediol, 19356-17-3, LGM PharmaCalcifediol, CAS number 19356-17-3 is essentially a man-made form of vitamin D. Calcifediol is crucial in helping patients to attain and maintain proper levels of calcium and phosphorus. Those patients with kidney disease may find the use of calcifediol advantageous, as it helps to keep calcium levels stable and allow normal bone growth. Marketed by Organon as Calderol, calcifediol is available in capsules to be taken orally, as either a 0.02 or a 0.05 milligram dose.

For patients with Psoriasis and Vitiligo, vitamin D analogues can be extremely efficacious:


Maxacalcitol, CAS number 103909-75-7
Maxacalcitol, 103909-75-7, LGM PharmaMaxacalcitol, CAS number 103909-75-7 is an anti-psoriatic vitamin D analogue, as well as a vitamin D3 analogue. In studies comparing maxacalcitol with either Calcipotriol or Tacalcitol, maxacalcitol proved to be a stronger opponent, offering a ten times greater efficacy at suppressing keratinocyte proliferation. One particular double-blind, randomized study involved a once-daily topical dose of maxacalcitol in patients with mild to moderate chronic plaque psoriasis. The concentrations of maxacalcitol ointment included 6, 12.5, 25 and 50 micrograms, with greatest effect noted for the 25 microgram dose. The 50 microgram once daily dose of calcipotriol ointment offered a comparative effect when compared to the 25 microgram dose of maxacalcitol, of which 55 percent of patients reported remarkable improvement in their psoriasis.

Calcipotriol CAS number 112965-21-6
Calcipotriol, 112965-21-6, LGM PharmaCalcipotriol CAS number 112965-21-6 continues to be a viable contender for skin conditions like vitiligo. Known as the brand name Dovonex, marketed by LEO Laboratories, Ltd., for Warner Chilcott, calcipotriol remains a respected topical dermatologic product. In The British Journal of Dermatology study results were published documenting the conclusions from a clinical trial, which determined the effectiveness and tolerability of calcipotriol cream, used as a monotherapy in conjunction with psoralen plus ultraviolet A (PUVA), in the treatment of vitiligo patients. Patients were treated with 50 micrograms twice-daily of topical calcipotriol monotherapy or twice-daily topical calcipotriol, 50 micrograms, along with topical or oral 8-methoxypsoralen PUVA three times weekly. Results were positive, with 77 percent of patients experiencing between a 30-100 percent marked improvement in their condition, with no recorded adverse effects. Those patients treated with the combination therapy also demonstrated improvement and indicated a positive response.

Tacalcitol CAS number 57333-96-7
Tacalcitol 57333-96-7Tacalcitol CAS number 57333-96-7 is another anti-psoriatic, synthetic vitamin D3 analogue. Marketed outside the U.S. under several names, including Curatoderm and Bonalfa, tacalcitol is a capable product. As plaque psoriasis is a skin disorder, caused by cells in the outer layer of the skin multiplying too quickly, tacalcitol is efficient and helps control the production of new skin cells when old cells die, thus controlling the effects of this condition.

With infrequent unfavorable effects, maxacalcitol, calcipotriol and tacalcitol are all prosperous products with great promise for the treatment of psoriasis and vitiligo.

Patients suffering from secondary hyperparathyroidism will find these antineoplastic API’s helpful:


Doxercalciferol, CAS number 54573-75-0
Doxercalciferol 54573-75-0Doxercalciferol, CAS number 54573-75-0, another synthetic analogue of vitamin D, offers potential antineoplastic activity for treatment of secondary hyperparathyroidism. Patients with low calcium concentrations find that their parathyroid gland secretes the parathyroid hormone, or PTH, which activates vitamin D in the body. By targeting osteoblasts to stimulate skeletal growth, doxercalciferol also acts on parathyroid glands to suppress PTH synthesis and secretion.

Paricalcitol, CAS number 131918-61-1
Paricalcitol 131918-61-1Paricalcitol, CAS number 131918-61-1 is also a noteworthy anti-hyperparathyroidism product. As an analog of calcitriol, the active form of vitamin D, it acts as an agonist for the calcitriol receptor and thus lowers the blood parathormone level. Also known as Zemplar, and marketed by Abbott laboratories, paricalcitol is utilized for the prevention and treatment of secondary hyperparathyroidism associated with chronic renal failure.

Both Paricalcitol and Doxercalciferol increase calcium absorption in the small intestine, and prove their efficacy not only by promoting the release of calcium from bones, but also reducing calcium excretion in the kidneys.

With the biology, as well as the gene regulatory properties of vitamin D more fully understood by researchers, the use and experimentation with vitamin D analogues are in the forefront of medical technology. The potential unique and designer formulations of the vitamin D analogues offer personalized therapeutic potential for patients suffering from secondary hyperparathyroidism, plaque psoriasis, vitiligo, calcium deficiences, as well as other autoimmune conditions related to a lack of vitamin D. The aforementioned patient populations stand to benefit greatly from these conceivable salubrious discoveries.

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

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