MVT-602

Human clinical Hormonal Health 3 sources

MVT-602 (formerly TAK-448) is a potent, long-acting kisspeptin receptor (KISS1R) agonist. Research shows it induces a prolonged luteinizing hormone (LH) surge compared to native kisspeptin, making it a promising candidate for treating female reproductive disorders like polycystic ovary syndrome (PCOS) and hypothalamic amenorrhea (HA), as well as for triggering oocyte maturation in in vitro fertilization (IVF).

01Dosing reference

Amount

0.1 - 3.0 mcg (single dose in clinical trials for ovulation induction)

Frequency

Single bolus (in current trial protocols)

Cycle

Administered once during the follicular phase or after ovarian stimulation

Reference figures, not a recommendationThese values reflect amounts described in the literature and vendor documentation this database indexes. Use the reconstitution calculator to convert them into syringe units.

02Mechanism of action

KISS1R Activation

MVT-602 binds to and activates the kisspeptin receptor (KISS1R) on gonadotropin-releasing hormone (GnRH) neurons in the hypothalamus.

GnRH Secretion

Activation of KISS1R stimulates the release of GnRH into the hypophyseal portal system.

Gonadotropin Surge

GnRH acts on the anterior pituitary to stimulate a robust and prolonged secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which are critical for ovulation and reproductive function.

03Human evidence

MVT-602 induced an LH surge of similar amplitude but longer duration compared to native kisspeptin-54 (KP54) in healthy premenopausal women.

Phase 1/2a randomized, placebo-controlled trials in healthy women, showing peak LH levels occurring later (around 21-24 hours) and remaining elevated longer.

In women with hypothalamic amenorrhea (HA), MVT-602 produced a more pronounced and rapid rise in gonadotropins (LH and FSH) compared to healthy women.

Clinical study comparing the endocrine response to a single subcutaneous bolus of MVT-602 in women with HA versus healthy women in the follicular phase.

MVT-602 successfully triggered ovulation in women undergoing minimal ovarian stimulation.

Phase 2a trial where ovulation occurred within 5 days in up to 100% of women receiving higher doses (3 μg) of MVT-602.

04Preclinical evidence

MVT-602 (TAK-448) demonstrated potent and full agonistic activity at the rat KISS1R, comparable to natural kisspeptin-10, but with enhanced in vivo stability.

In vitro receptor binding and calcium mobilization assays.

Continuous subcutaneous administration of TAK-448 in male rats initially increased testosterone, followed by a rapid and profound suppression to castrate levels.

Preclinical studies evaluating TAK-448 for androgen deprivation therapy in prostate cancer models, showing more rapid testosterone suppression than the GnRH agonist leuprolide.

05What is known vs. unknown

Reasonably established

MVT-602 has a longer half-life (1.5-2.2 hours) compared to native kisspeptin-54 (0.5 hours).
It can induce a prolonged LH surge that mimics the physiological mid-cycle surge necessary for ovulation.
It is well-tolerated in human trials with no serious adverse effects reported across tested dose ranges.
It shows potential as an oocyte maturation trigger in IVF, potentially reducing the risk of ovarian hyperstimulation syndrome (OHSS).

Unknowns & limits

The optimal dosing regimen for repeated administration in chronic anovulatory conditions like HA remains to be fully established.
Long-term safety and efficacy data in large-scale Phase 3 clinical trials are not yet available.
Its role in prostate cancer treatment was explored but development for this indication appears to have been discontinued or deprioritized compared to female infertility.

06Safety & regulatory context

Regulatory statusMVT-602 has been shown to be safe and well-tolerated in Phase 1 and Phase 2 clinical trials in healthy women and those with reproductive disorders. Reported adverse events were similar to placebo with no apparent dose-related effects. Because it acts upstream in the HPG axis, it is thought to carry a lower risk of causing ovarian hyperstimulation syndrome (OHSS) compared to traditional hCG triggers used in IVF. It is currently an investigational drug and is not FDA-approved for any indication.

07Compared with Kisspeptin-54 (KP54)

MVT-602 vs. Kisspeptin-54 (KP54)

Key difference

MVT-602 is a synthetic analog with a modified structure that confers a longer half-life and induces a more prolonged LH surge compared to the native KP54 peptide.

When researchers discuss each

KP54 is often discussed in the context of natural physiological regulation and early proof-of-concept studies for kisspeptin therapeutics. MVT-602 is discussed when evaluating advanced clinical candidates designed to overcome the short half-life and potential tachyphylaxis associated with native kisspeptin administration.

08Glossary

Kisspeptin

A neuropeptide that plays a crucial role in initiating the release of reproductive hormones by stimulating GnRH neurons.

Hypothalamic Amenorrhea (HA)

A condition where menstruation stops due to a problem in the hypothalamus, often linked to stress, weight loss, or excessive exercise, resulting in low reproductive hormone levels.

Luteinizing Hormone (LH) Surge

A rapid increase in LH levels that triggers the release of a mature egg from the ovary (ovulation).

Agonist

A substance that binds to a receptor and activates it to produce a biological response.

09Knowledge check

Q1What is the primary advantage of MVT-602 over native kisspeptin-54 (KP54) in clinical applications?

Q2In preclinical studies on male rats, what was the effect of continuous administration of TAK-448 (MVT-602)?

Q3Which interpretation best matches the limits of the current human clinical evidence for MVT-602 as described in the dossier?

Q4According to the dossier, in what contexts are researchers most likely to discuss native kisspeptin-54 (KP54) versus MVT-602?

Q5Which statement about MVT-602's safety and regulatory status is supported by the dossier?

10Sources

More in Hormonal Health

See all

Kisspeptin-10

Hormonal Health

Human clinical

Kisspeptin-10 is a potent neuropeptide that acts as an upstream regulator of the hypothalamic-pituitary-gonadal (HPG) axis. Research shows it stimulates the release of gonadotropin-releasing hormone (GnRH), subsequently increasing luteinizing hormone (LH), follicle-stimulating hormone (FSH), and testosterone levels. It is heavily studied for its potential in treating infertility, hypogonadism, and reproductive disorders.

100-300 mcg per dose

Gonadorelin

Hormonal Health

FDA-approved context

Gonadorelin is a synthetic version of gonadotropin-releasing hormone (GnRH). It stimulates the anterior pituitary gland to release luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which in turn stimulate the gonads to produce testosterone and sperm in males, and estrogen and eggs in females.

100-200 mcg per dose

hCG (Human Chorionic Gonadotropin)

Hormonal Health

FDA-approved context

hCG is a hormone naturally produced during pregnancy that mimics luteinizing hormone (LH) in the body. In research and clinical settings, it is widely used to stimulate testosterone production, preserve fertility, and treat hypogonadism in men, as well as to induce ovulation in women.

250-500 IU

Research and educational use onlyNothing on this site is medical advice, a prescription, or a recommendation for human use. Compounds documented here are research chemicals. Consult a qualified clinician before making any health decision.